Target Information

Target General Information

Top

Target ID

T78709 (Former ID: TTDS00098)

Target Name

5-HT 1A receptor (HTR1A)

Synonyms

Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A

Gene Name

HTR1A

Target Type

Successful target

[1]

Disease

[+] 5 Target-related Diseases

Anxiety disorder [ICD-11: 6B00-6B0Z]

Depression [ICD-11: 6A70-6A7Z]

Hypertension [ICD-11: BA00-BA04]

Migraine [ICD-11: 8A80]

Mood disorder [ICD-11: 6A60-6E23]

Function

Functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).

Click to Show/Hide

BioChemical Class

GPCR rhodopsin

UniProt ID

5HT1A_HUMAN

Sequence

MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC
TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED
RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT
RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN
SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP
FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC
RQ

Click to Show/Hide

3D Structure

Click to Show 3D Structure of This Target

AlphaFold

HIT2.0 ID

T31QEZ

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 8 Approved Drugs

Buspirone

Drug Info

Approved

Anxiety disorder

[2], [3]

Flibanserin

Drug Info

Approved

Mood disorder

[4], [5]

OPC-34712

Drug Info

Approved

Major depressive disorder

[6], [7]

TERTATOLOL

Drug Info

Approved

Hypertension

[8], [9]

Trazodone

Drug Info

Approved

Depression

[10], [11]

Treximet

Drug Info

Approved

Migraine

[12]

Urapidil

Drug Info

Approved

Hypertension

[9]

Vilazodone

Drug Info

Approved

Major depressive disorder

[13], [14]

Clinical Trial Drug(s)

[+] 32 Clinical Trial Drugs

CM-2395

Drug Info

Phase 3

Schizophrenia

[15]

Eltoprazine

Drug Info

Phase 3

Attention deficit hyperactivity disorder

[16]

SEP-363856

Drug Info

Phase 3

Schizophrenia

[17]

Xaliproden

Drug Info

Phase 3

Juvenile idiopathic arthritis

[18]

LECOZOTAN HYDROCHLORIDE

Drug Info

Phase 2/3

Cognitive impairment

[19]

Sarizotan

Drug Info

Phase 2/3

Rett syndrome

[20]

Ensaculin hydrochloride

Drug Info

Phase 2

Parkinson disease

[21]

FKW00GA

Drug Info

Phase 2

Social phobia

[16]

Mazapertine succinate

Drug Info

Phase 2

Psychotic disorder

[22]

MIN-117

Drug Info

Phase 2

Major depressive disorder

[23]

MN-305

Drug Info

Phase 2

Mood disorder

[24]

Neu-P11

Drug Info

Phase 2

Insomnia

[25]

OPC-14523

Drug Info

Phase 2

Mood disorder

[26]

ORG-13011

Drug Info

Phase 2

Psychotic disorder

[27]

RP5063

Drug Info

Phase 2

Schizophrenia

[28]

S-15535

Drug Info

Phase 2

Anxiety disorder

[29], [30]

S-16924

Drug Info

Phase 2

Anxiety disorder

[31], [32], [33]

SDZ-MAR-327

Drug Info

Phase 2

Psychotic disorder

[34], [35]

SUN N4057

Drug Info

Phase 2

Coronary artery disease

[36]

TGBA01AD

Drug Info

Phase 2

Mood disorder

[24]

TGFK08AA

Drug Info

Phase 2

Generalized anxiety disorder

[37]

TGFK09SD

Drug Info

Phase 2

Hypoactive sexual desire dysfunction

[38]

TGWOOAA

Drug Info

Phase 2

Social phobia

[39]

Zalospirone

Drug Info

Phase 2

Anxiety disorder

[40], [41]

1192U90

Drug Info

Phase 1

Psychotic disorder

[42]

AV-965

Drug Info

Phase 1

Alzheimer disease

[43]

DSP-1053

Drug Info

Phase 1

Major depressive disorder

[44]

GSK-958108

Drug Info

Phase 1

Premature ejaculation

[45]

NLX-101

Drug Info

Phase 1

Rett syndrome

[46]

SKL-PSY

Drug Info

Phase 1

Bipolar disorder

[47]

SSR-181507

Drug Info

Phase 1

Schizophrenia

[34]

Umespirone

Drug Info

Phase 1

Anxiety disorder

[48]

Patented Agent(s)

[+] 5 Patented Agents

PMID30124346-Compound-13TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[49]

PMID30124346-Compound-34TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[49]

PMID30124346-Compound-60TABLE5

Drug Info

Patented

Parkinson disease

[49], [50], [51]

PMID30124346-Compound-LDT66

Drug Info

Patented

Benign prostatic hyperplasia

[49]

PMID30124346-Compound-LDT8

Drug Info

Patented

Benign prostatic hyperplasia

[49]

Discontinued Drug(s)

[+] 36 Discontinued Drugs

LYSERGIC ACID DIETHYLAMIDE

Drug Info

Withdrawn from market

Addictive disorder

[52], [53]

Bifeprunox

Drug Info

Discontinued in Phase 3

Schizophrenia

[34]

BMS-181100

Drug Info

Discontinued in Phase 3

Psychotic disorder

[54], [55]

Flesinoxan

Drug Info

Discontinued in Phase 3

Anxiety disorder

[56], [57]

Adatanserin

Drug Info

Discontinued in Phase 2

Mood disorder

[24]

ALNESPIRONE

Drug Info

Discontinued in Phase 2

Anxiety disorder

[58]

AP-521

Drug Info

Discontinued in Phase 2

Anxiety disorder

[59]

DU 125530

Drug Info

Discontinued in Phase 2

Mood disorder

[60]

GSK163090

Drug Info

Discontinued in Phase 2

Anxiety disorder

[61]

LESOPITRON DIHYDROCHLORIDE

Drug Info

Discontinued in Phase 2

Mood disorder

[62]

PRX-00023

Drug Info

Discontinued in Phase 2

Mood disorder

[24]

REC-15/3079

Drug Info

Discontinued in Phase 2

Urinary incontinence

[63], [64]

Robalzotan

Drug Info

Discontinued in Phase 2

Anxiety disorder

[65], [66]

BINOSPIRONE MESYLATE

Drug Info

Discontinued in Phase 1

Anxiety disorder

[67]

DU-29894

Drug Info

Discontinued in Phase 1

Psychotic disorder

[68]

E2101

Drug Info

Discontinued in Phase 1

Spasm

[69]

Ebalzotan

Drug Info

Discontinued in Phase 1

Anxiety disorder

[70]

Eptapirone

Drug Info

Discontinued in Phase 1

Anxiety disorder

[71]

GR-127607

Drug Info

Discontinued in Phase 1

Migraine

[72]

Nerisopam

Drug Info

Discontinued in Phase 1

Anxiety disorder

[73]

SLV-313

Drug Info

Discontinued in Phase 1

Schizophrenia

[34]

SUN-8399

Drug Info

Discontinued in Phase 1

Anxiety disorder

[74]

U-93385

Drug Info

Discontinued in Phase 1

Anxiety disorder

[75]

A-74283

Drug Info

Terminated

Hypertension

[77]

Anpirtoline

Drug Info

Terminated

Pain

[78]

BTS-79018

Drug Info

Terminated

Schizophrenia

[34]

CGS-18102A

Drug Info

Terminated

Anxiety disorder

[79]

Du-123015

Drug Info

Terminated

Anxiety disorder

[80]

Gepirone

Drug Info

Terminated

Depression

[24]

HT-90B

Drug Info

Terminated

Anxiety disorder

[81]

Ipsapirone

Drug Info

Terminated

Anxiety disorder

[82], [83]

LY-293284

Drug Info

Terminated

Anxiety disorder

[84], [85]

RWJ-25730

Drug Info

Terminated

Psychotic disorder

[86]

S-14506

Drug Info

Terminated

Anxiety disorder

[87], [88]

SLV-307

Drug Info

Terminated

Parkinson disease

[89]

WAY-100635

Drug Info

Terminated

Eating disorder

[90], [91]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

CM-2236

Drug Info

Preclinical

Post-traumatic stress disorder

[76]

PD-158771

Drug Info

Preclinical

Schizophrenia

[34]

Mode of Action

[+] 7 Modes of Action

Agonist

[+] 50 Agonist drugs

Buspirone

Drug Info

[1]

Urapidil

Drug Info

[97]

CM-2395

Drug Info

[98]

Eltoprazine

Drug Info

[99]

SEP-363856

Drug Info

[20]

MN-305

Drug Info

[24]

Neu-P11

Drug Info

[105]

SUN N4057

Drug Info

[113]

Zalospirone

Drug Info

[41]

1192U90

Drug Info

[34]

Aryl piperazine derivative 14

Drug Info

[49]

Aryl piperazine derivative 15

Drug Info

[49]

Aryl piperazine derivative 16

Drug Info

[49]

PMID30124346-Compound-13TABLE4

Drug Info

[49]

Flesinoxan

Drug Info

[129]

Adatanserin

Drug Info

[24], [132]

ALNESPIRONE

Drug Info

[133], [9]

AP-521

Drug Info

[134], [9]

LESOPITRON DIHYDROCHLORIDE

Drug Info

[136]

Ebalzotan

Drug Info

[144]

Eptapirone

Drug Info

[145]

GR-127607

Drug Info

[146]

Nerisopam

Drug Info

[147]

SUN-8399

Drug Info

[149]

U-93385

Drug Info

[150], [9]

CM-2236

Drug Info

[151]

A-74283

Drug Info

[152]

Gepirone

Drug Info

[24]

Ipsapirone

Drug Info

[159]

LY-293284

Drug Info

[160]

1-naphthylpiperazine

Drug Info

[184], [173]

5-CT

Drug Info

[199]

7-methoxy-1-naphthylpiperazine

Drug Info

[184]

BRL-15572

Drug Info

[203]

CP 93129

Drug Info

[199]

EDMT

Drug Info

[206]

FG-5893

Drug Info

[210]

L-772,405

Drug Info

[212]

LP-12

Drug Info

[213]

LP-211

Drug Info

[214]

LP-44

Drug Info

[213]

LY 165,163

Drug Info

[210]

nafadotride

Drug Info

[210]

piribedil

Drug Info

[221]

S-14671

Drug Info

[111]

SB 216641

Drug Info

[203]

spiroxatrine

Drug Info

[210]

U92016A

Drug Info

[231]

[3H]8-OH-DPAT

Drug Info

[236]

[3H]NLX-112

Drug Info

[237]

Modulator

[+] 34 Modulator drugs

Flibanserin

Drug Info

[5]

OPC-34712

Drug Info

[92], [93]

Trazodone

Drug Info

[95]

Vilazodone

Drug Info

[14]

Sarizotan

Drug Info

[102]

Ensaculin hydrochloride

Drug Info

[21], [103]

FKB01MD

Drug Info

[16]

Mazapertine succinate

Drug Info

[102]

OPC-14523

Drug Info

[106]

S-16924

Drug Info

[32], [33]

SDZ-MAR-327

Drug Info

[112]

TGBA01AD

Drug Info

[114]

TGFK08AA

Drug Info

[115]

TGFK09SD

Drug Info

[116]

NLX-101

Drug Info

[121]

SKL-PSY

Drug Info

[122]

SSR-181507

Drug Info

[123]

Bifeprunox

Drug Info

[126]

BMS-181100

Drug Info

[127], [128]

PRX-00023

Drug Info

[138]

DU-29894

Drug Info

[142]

E2101

Drug Info

[143]

SLV-313

Drug Info

[148]

Anpirtoline

Drug Info

[78]

CGS-18102A

Drug Info

[155]

Du-123015

Drug Info

[157]

HT-90B

Drug Info

[158]

RWJ-25730

Drug Info

[162]

S-14506

Drug Info

[163]

CGS-19480A

Drug Info

[204], [9]

EMD 56551

Drug Info

[207]

NPT-500

Drug Info

[122]

SEL-73

Drug Info

[122]

SR-59026

Drug Info

[230]

Inhibitor

[+] 142 Inhibitor drugs

TERTATOLOL

Drug Info

[94]

LYSERGIC ACID DIETHYLAMIDE

Drug Info

[125]

Sunepitron

Drug Info

[130]

TIOSPIRONE

Drug Info

[131]

MAZAPERTINE

Drug Info

[137]

A-80426

Drug Info

[153]

BMY-7378

Drug Info

[154]

CP-293019

Drug Info

[156]

WB-4101

Drug Info

[168]

(3-Chloro-phenyl)-piperazin-1-yl-methanone

Drug Info

[169]

(R)-(-)-10-methyl-11-hydroxyaporphine

Drug Info

[170]

(R)-11-Amino-2-methoxyaporphine

Drug Info

[171]

(R)-2,11-Diaminoaporphine

Drug Info

[171]

1,2,3,4-Tetrahydro-naphthalen-2-ylamine

Drug Info

[173]

1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane

Drug Info

[174]

1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane

Drug Info

[174]

1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane

Drug Info

[174]

1,6-bis(4-m-tolylpiperazin-1-yl)hexane

Drug Info

[174]

1,6-bis(4-phenylpiperazin-1-yl)hexane

Drug Info

[174]

1-((S)-2-aminopropyl)-1H-indazol-6-ol

Drug Info

[175]

1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine

Drug Info

[169]

1-(2,5-Dimethoxy-phenyl)-piperazine

Drug Info

[169]

1-(2,5-dimethoxyphenyl)propan-2-amine

Drug Info

[176]

1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine

Drug Info

[177]

1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine

Drug Info

[178]

1-(2-(2-fluorobenzyloxy)phenyl)piperazine

Drug Info

[177]

1-(2-(3-fluorophenoxy)phenyl)piperazine

Drug Info

[177]

1-(2-(4-fluorophenoxy)phenyl)piperazine

Drug Info

[177]

1-(2-(benzyloxy)phenyl)piperazine

Drug Info

[177]

1-(2-(phenoxymethyl)phenyl)piperazine

Drug Info

[177]

1-(2-Butoxy-phenyl)-piperazine

Drug Info

[179]

1-(2-Chloro-phenyl)-piperazine

Drug Info

[180]

1-(2-Ethoxy-phenyl)-piperazine

Drug Info

[179]

1-(2-Fluoro-phenyl)-piperazine

Drug Info

[179]

1-(2-Isopropoxy-phenyl)-piperazine

Drug Info

[179]

1-(2-Methoxy-phenyl)-4-propyl-piperazine

Drug Info

[181]

1-(2-Methoxy-phenyl)-piperazine

Drug Info

[180]

1-(2-methoxyphenyl)-4-pentylpiperazine

Drug Info

[182]

1-(2-phenoxyphenyl)piperazine

Drug Info

[177]

1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine

Drug Info

[183]

1-(3-Fluoro-phenyl)-piperazine

Drug Info

[179]

1-(3-Nitro-phenyl)-piperazine

Drug Info

[179]

1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine

Drug Info

[169]

1-(7-Methoxy-naphthalen-2-yl)-piperazine

Drug Info

[184]

1-(benzyloxy)-2-(2-phenylethyl)benzene

Drug Info

[185]

1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene

Drug Info

[185]

1-Benzyl-4-chroman-2-ylmethyl-piperazine

Drug Info

[186]

1-Butyl-4-(2-methoxy-phenyl)-piperazine

Drug Info

[181]

1-Ethyl-4-(2-methoxy-phenyl)-piperazine

Drug Info

[181]

1-Methyl-1,3-dihydro-indol-2-one

Drug Info

[187]

1-Naphthalen-2-yl-piperazine

Drug Info

[173]

1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine

Drug Info

[188]

1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene

Drug Info

[185]

2-(2'-methyl-biphenyl-3-yl)-ethylamine

Drug Info

[189]

2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol

Drug Info

[176]

2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[178]

2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[178]

2-(2-Methoxy-phenyl)-1-methyl-ethylamine

Drug Info

[176]

2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[178]

2-(3-Bromophenylthio)-N,N-dimethylethanamine

Drug Info

[190]

2-(3-Methoxy-phenyl)-1-methyl-ethylamine

Drug Info

[176]

2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one

Drug Info

[186]

2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine

Drug Info

[176]

2-(4-Bromo-phenyl)-1-methyl-ethylamine

Drug Info

[176]

2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine

Drug Info

[191]

2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine

Drug Info

[192]

2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine

Drug Info

[190]

2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol

Drug Info

[94]

2-phenoxy-3-(piperidin-4-yl)pyridine

Drug Info

[178]

2-Piperazin-1-yl-benzonitrile

Drug Info

[179]

2-Piperazin-1-yl-phenol

Drug Info

[169]

2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine

Drug Info

[185]

3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole

Drug Info

[193]

3-(1-Propyl-pyrrolidin-3-yl)-phenol

Drug Info

[188]

3-(2-Amino-propyl)-1H-indol-5-ol

Drug Info

[192]

3-(2-Benzylamino-ethoxy)-phenol

Drug Info

[194]

3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine

Drug Info

[188]

3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one

Drug Info

[186]

3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one

Drug Info

[186]

3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine

Drug Info

[178]

3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one

Drug Info

[169]

3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol

Drug Info

[195]

3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol

Drug Info

[195]

3-Naphthalen-1-yl-1-propyl-pyrrolidine

Drug Info

[188]

3-Naphthalen-1-yl-pyrrolidine

Drug Info

[188]

3-Phenyl-1-propyl-pyrrolidine

Drug Info

[188]

3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine

Drug Info

[185]

4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol

Drug Info

[196]

4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine

Drug Info

[177]

4-(2-(2-fluorobenzyloxy)phenyl)piperidine

Drug Info

[177]

4-(2-(3-chlorophenoxy)phenyl)piperidine

Drug Info

[177]

4-(2-(3-fluorophenoxy)phenyl)piperidine

Drug Info

[177]

4-(2-(4-fluorobenzyloxy)phenyl)piperidine

Drug Info

[177]

4-(2-(4-fluorophenoxy)phenyl)piperidine

Drug Info

[177]

4-(2-(benzyloxy)-3-fluorophenyl)piperidine

Drug Info

[177]

4-(2-(benzyloxy)-6-fluorophenyl)piperidine

Drug Info

[177]

4-(2-(benzyloxy)phenyl)piperidine

Drug Info

[177]

4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine

Drug Info

[178]

4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine

Drug Info

[177]

100

4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine

Drug Info

[177]

101

4-(2-fluoro-6-phenoxyphenyl)piperidine

Drug Info

[177]

102

4-(2-phenoxyphenyl)piperidine

Drug Info

[177]

103

4-(3-fluoro-2-phenoxyphenyl)piperidine

Drug Info

[177]

104

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[197]

105

4-Benzyl-1-chroman-2-ylmethyl-piperidine

Drug Info

[186]

106

4-Benzyl-1-chroman-3-ylmethyl-piperidine

Drug Info

[186]

107

5,6-dichloro-3,4-dihydroquinazolin-2-amine

Drug Info

[198]

108

5-chloro-3,4-dihydroquinazolin-2-amine

Drug Info

[198]

109

5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine

Drug Info

[198]

110

5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine

Drug Info

[198]

111

8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine

Drug Info

[94]

112

8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline

Drug Info

[173]

113

8-Methoxy-2-piperazin-1-yl-quinoline

Drug Info

[173]

114

8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine

Drug Info

[198]

115

8-Methoxy-quinolin-2-ylamine

Drug Info

[173]

116

9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine

Drug Info

[94]

117

A-987306

Drug Info

[201]

118

AGROCLAVINE

Drug Info

[202]

119

Brolamfetamine

Drug Info

[176]

120

CHLOROPHENYLPIPERAZINE

Drug Info

[179]

121

ESCHOLTZINE

Drug Info

[208]

122

Etisulergine

Drug Info

[209]

123

JNJ-10392980

Drug Info

[211]

124

MCL-516

Drug Info

[171]

125

N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine

Drug Info

[196]

126

N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine

Drug Info

[196]

127

N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide

Drug Info

[214]

128

N-methyllaurotetanine

Drug Info

[208]

129

N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide

Drug Info

[216]

130

PB-28

Drug Info

[219]

131

PG-01037

Drug Info

[220]

132

PHENYLPIPERAZINE

Drug Info

[173]

133

QUIPAZINE

Drug Info

[222]

134

SB-271046

Drug Info

[227]

135

SB-656104

Drug Info

[228]

136

SEROTONIN

Drug Info

[222]

137

SNAP-8719

Drug Info

[229]

138

TFMPP

Drug Info

[169]

139

UH-232

Drug Info

[232]

140

UH-301

Drug Info

[233]

141

WAY-466

Drug Info

[234]

142

[3H]spiperone

Drug Info

[168]

Antagonist

[+] 41 Antagonist drugs

Treximet

Drug Info

[96]

Xaliproden

Drug Info

[100]

LECOZOTAN HYDROCHLORIDE

Drug Info

[9], [101]

FKW00GA

Drug Info

[16]

MIN-117

Drug Info

[104]

ORG-13011

Drug Info

[9], [107]

RP5063

Drug Info

[108], [109]

S-15535

Drug Info

[9], [110], [111]

TGWOOAA

Drug Info

[117]

AV-965

Drug Info

[118]

DSP-1053

Drug Info

[119]

GSK-958108

Drug Info

[120]

Umespirone

Drug Info

[124]

PMID30124346-Compound-LDT8

Drug Info

[49]

DU 125530

Drug Info

[135]

GSK163090

Drug Info

[96]

REC-15/3079

Drug Info

[139]

Robalzotan

Drug Info

[140]

BINOSPIRONE MESYLATE

Drug Info

[141], [9]

PD-158771

Drug Info

[34]

NAN-190

Drug Info

[161]

SDZ 216-525

Drug Info

[161]

SLV-307

Drug Info

[164]

WAY-100635

Drug Info

[135], [165], [166], [167]

(R)-flurocarazolol

Drug Info

[172]

(S)-flurocarazolol

Drug Info

[172]

9-OH-risperidone

Drug Info

[200]

cyamemazine

Drug Info

[205]

GR 125,743

Drug Info

[199]

LY433221

Drug Info

[215]

MPDT

Drug Info

[206]

P-MPPI

Drug Info

[217], [161]

p-[18F]MPPF

Drug Info

[218]

repinotan

Drug Info

[223]

SB 272183

Drug Info

[225]

SB 649915

Drug Info

[226]

SB 714786

Drug Info

[226]

WAY 100135

Drug Info

[161]

[11C]WAY100635

Drug Info

[235]

[3H]p-MPPF

Drug Info

[238]

[3H]robalzotan

Drug Info

[239]

Ligand

[+] 4 Ligand drugs

Aryl piperazine derivative 1

Drug Info

[49]

Aryl piperazine derivative 6

Drug Info

[49]

PMID30124346-Compound-34TABLE4

Drug Info

[49]

PMID30124346-Compound-60TABLE5

Drug Info

[49]

Binder

[+] 1 Binder drugs

BTS-79018

Drug Info

[34]

Modulator (allosteric modulator)

[+] 1 Modulator (allosteric modulator) drugs

RS-30199

Drug Info

[224]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

Top

Target-regulating Transcription Factors

Target-regulating Transcription Factors Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 3 KEGG Pathways

cAMP signaling pathway

Neuroactive ligand-receptor interaction

Serotonergic synapse

Panther Pathway

[+] 2 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway

5HT1 type receptor mediated signaling pathway

Reactome

[+] 2 Reactome Pathways

Serotonin receptors

G alpha (i) signalling events

WikiPathways

[+] 6 WikiPathways

Serotonin HTR1 Group and FOS Pathway

SIDS Susceptibility Pathways

Monoamine GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

REF 1

Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.

REF 2

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 36).

REF 3

Glutamate and anxiety disorders. Curr Psychiatry Rep. 2007 Aug;9(4):278-83.

REF 4

REF 5

Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.

REF 6

REF 7

ClinicalTrials.gov (NCT01397786) Safety and Tolerability Study of Oral OPC-34712 as Maintenance Treatment in Adults With Schizophrenia. U.S. National Institutes of Health.

REF 8

REF 9

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 10

REF 11

Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.

REF 12

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021926.

REF 13

REF 14

2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.

REF 15

Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010.

REF 16

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 17

ClinicalTrials.gov (NCT04109950) A Clinical Study to Evaluate the Long-term Safety and Tolerability of an Investigational Drug in People With Schizophrenia. U.S. National Institutes of Health.

REF 18

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 19

ClinicalTrials.gov (NCT00277810) Study Evaluating the Safety, Tolerability, and Efficacy of Lecozotan SR in Outpatients With Alzheimer's Disease. U.S. National Institutes of Health.

REF 20

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 21

Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58.

REF 22

Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. J Med Chem. 1998 Jun 4;41(12):1997-2009.

REF 23

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037483)

REF 24

Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.

REF 25

ClinicalTrials.gov (NCT01489969) Sleep Laboratory Study to Investigate the Safety and Efficacy of Neu-P11 in Primary Insomnia Patients. U.S. National Institutes of Health.

REF 26

Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66.

REF 27

ClinicalTrials.gov (NCT00000189) Gepirone vs Placebo in Treatment of Cocaine Dependence - 3. U.S. National Institutes of Health.

REF 28

ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health.

REF 29

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002186)

REF 31

REF 32

S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther. 1998 Sep;286(3):1341-55.

REF 33

S-16924 [(R)-2-[1-[2-(2,3-dihydro-benzo[1,4]dioxin-5-yloxy)-ethyl]- pyrrolidin-3yl]-1-(4-fluorophenyl)-ethanone], a novel, potential antipsychotic with marked serotonin1A agonist properties: III. Anxiolytic actions in comparison with clozapine and haloperidol. J Pharmacol Exp Ther. 1999 Mar;288(3):1002-14.

REF 34

The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.

REF 35

Positron emission tomographic analysis of central dopamine D1 receptor binding in normal subjects treated with the atypical neuroleptic, SDZ MAR 327. Int J Mol Med. 1998 Jan;1(1):243-7.

REF 36

ClinicalTrials.gov (NCT00272909) Efficacy of SUN N4057 in Subjects With Acute Ischemic Stroke and Measurable Penumbra on Magnetic Resonance Imaging (MRI). U.S. National Institutes of Health.

REF 37

Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.

REF 38

Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.

REF 39

Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.

REF 40

REF 41

The serotonin 5-HT receptor agonist tandospirone improves executive function in common marmosets. Behav Brain Res. 2015 Jul 1;287:120-6.

REF 42

1192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42.

REF 43

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412)

REF 44

ClinicalTrials.gov (NCT01774747) A Multiple Ascending Oral Dose Evaluation of the Safety, Tolerability, and Pharmacokinetics of DSP-1053 and Its Metabolites in Healthy Subjects and in Subjects With Major Depressive Disorder. U.S. National Institutes of Health.

REF 45

ClinicalTrials.gov (NCT00664365) FTIH Study With GSK958108. U.S. National Institutes of Health.

REF 46

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 47

Clinical pipeline report, company report or official report of SK Biopharmaceuticals.

REF 48

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000698)

REF 49

5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.

REF 50

mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.

REF 51

Caspase inhibitors: a review of recently patented compounds (2013-2015).Expert Opin Ther Pat. 2018 Jan;28(1):47-59.

REF 52

REF 53

Psychopathology and psychophysiology of minimal LSD-25 dosage; a preliminary dosage-response spectrum. AMA Arch Neurol Psychiatry. 1958 Feb;79(2):208-10.

REF 54

REF 55

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000679)

REF 56

REF 57

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001126)

REF 58

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001421)

REF 59

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004776)

REF 60

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014469)

REF 61

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026154)

REF 62

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001441)

REF 63

REF 64

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010455)

REF 65

REF 66

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006370)

REF 67

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000677)

REF 68

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001422)

REF 69

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013610)

REF 70

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006909)

REF 71

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010848)

REF 72

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531)

REF 73

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001415)

REF 74

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001433)

REF 75

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002172)

REF 76

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029346)

REF 77

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002258)

REF 78

Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Nucl Med Biol. 2006 Apr;33(3):325-32.

REF 79

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001927)

REF 80

Neither in vivo MRI nor behavioural assessment indicate therapeutic efficacy for a novel 5HT1A agonist in rat models of ischaemic stroke. BMC Neuroscience 2009, 10:82.

REF 81

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003558)

REF 82

REF 83

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000695)

REF 84

REF 85

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003567)

REF 86

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001430)

REF 87

REF 88

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001368)

REF 89

Pharmacokinetics, Pharmacodynamics and Tolerance of SLV 307 After Single Oral Administration in Healthy Male Volunteers. Clinical Pharmacology &#38 Therapeutics. 02/1999; 65(2).

REF 90

REF 91

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002783)

REF 92

Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.

REF 93

Brexpiprazole: First Global Approval.Drugs.2015 Sep;75(14):1687-97.

REF 94

Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).

REF 95

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 96

Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).

REF 97

Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.

REF 98

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)

REF 99

Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.

REF 100

Pharma & Vaccines. Product Development Pipeline. April 29 2009.

REF 101

A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in... Clin Pharmacol Ther. 2008 Jan;83(1):86-96.

REF 102

Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.Curr Med Chem.2014;21(4):437-57.

REF 103

The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component. Pharmacol Biochem Behav. 1998 Jul;60(3):703-7.

REF 104

Company report (Minerva Neurosciences),MIN-101,Schizophrenia, 6 trials completed; Once a day formulation completed , Phase IIa completed; Phase IIb enrollment ongoing and expected to continue over the last 3 quarters of 2015.

REF 105

Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.

REF 106

Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88.

REF 107

Antagonism of the 5-HT1A receptor stimulus in a conditioned taste aversion procedure. Eur Neuropsychopharmacol. 1999 Jun;9(4):345-9.

REF 108

Drug Development in Schizophrenia: Summary and Table. Pharmaceutical Medicine October 2014, Volume 28, Issue 5, pp 265-271

REF 109

EFFICACY AND SAFETY OF NOVEL DOPAMINE SEROTONIN STABILIZER RP 5063 IN ACUTE SCHIZOPHRENIA AND SCHIZOAFFECTIVE DISORDER. Schizophrenia Research Volume 153, Supplement 1, April 2014, Pages S22.

REF 110

S 15535, a benzodioxopiperazine acting as presynaptic agonist and postsynaptic 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine. Br J Pharmacol. 1999 Nov;128(6):1207-14.

REF 111

Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn Schmiedebergs Arch Pharmacol. 1998 Mar;357(3):205-17.

REF 112

DOI: 10.1038/sj.mp.4002062

REF 113

Experimental study of pharmacological hypothermia: enhanced neuroprotective effect of a novel 5-HT 1 A agonist SUN N4057 by the pharmacological hypothermia. No To Shinkei. 2001 Sep;53(9):853-8.

REF 114

Company report (Fabrekramer)

REF 115

50 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87.

REF 116

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032503)

REF 117

Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.

REF 118

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412)

REF 119

DSP-1053, a novel serotonin reuptake inhibitor with 5-HT1A partial agonistic activity, displays fast antidepressant effect with minimal undesirable effects in juvenile rats. Pharmacol Res Perspect. 2015 Jun;3(3):e00142.

REF 120

Clinical pipeline report, company report or official report of GlaxoSmithKline.

REF 121

In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat.Psychopharmacology (Berl).2012 May;221(2):261-72.

REF 122

REF 123

SSR181507, a dopamine D receptor and 5-HT() receptor ligand: evidence for mixed anxiolytic- and antidepressant-like activities.Pharmacol Biochem Behav.2011 Jan;97(3):428-35.

REF 124

The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacol Biochem Behav. 1991 Sep;40(1):89-96.

REF 125

Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes. J Med Chem. 1995 Mar 17;38(6):958-66.

REF 126

Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Addict Biol.2012 Mar;17(2):274-86.

REF 127

BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology. 1994 Feb;10(1):37-40.

REF 128

The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat

REF 129

Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission. Eur Neuropsychopharmacol. 1999 Sep;9(5):427-40.

REF 130

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.

REF 131

Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. J Med Chem. 1991 Nov;34(11):3316-28.

REF 132

Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents. J Med Chem. 1999Dec 16;42(25):5077-94.

REF 133

Chronic alnespirone-induced desensitization of somatodendritic 5-HT1A autoreceptors in the rat dorsal raphe nucleus. Eur J Pharmacol. 1999 Jan 22;365(2-3):165-73.

REF 134

The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats. J Pharmacol Sci. 2015 Jan;127(1):109-16.

REF 135

5-Hydroxytryptamine1A receptor occupancy by novel full antagonist 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-dioxide: a[11C][O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans. J Pharmacol Exp Ther. 2002 Jun;301(3):1144-50.

REF 136

Effect of acute administration of the 5-HT1A receptor ligand, lesopitron, on rat cortical 5-HT and dopamine turnover. Br J Pharmacol. 1994 Oct;113(2):425-30.

REF 137

A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.

REF 138

PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety.Pharmacol Biochem Behav.2009 Nov;94(1):8-15.

REF 139

N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract. JPharmacol Exp Ther. 2001 Dec;299(3):1027-37.

REF 140

Use of PET and the radioligand [carbonyl-(11)C]WAY-100635 in psychotropic drug development. Nucl Med Biol. 2000 Jul;27(5):515-21.

REF 141

Quantifying the 5-HT1A agonist action of buspirone in man. Psychopharmacology (Berl). 2001 Nov;158(3):224-9.

REF 142

A comparison of the neuro-endocrinological and temperature effects of DU 29894, flesinoxan, sulpiride and haloperidol in normal volunteers. Br J Clin Pharmacol. 1995 Jan;39(1):7-14.

REF 143

In vitro interactions between a potential muscle relaxant E2101 and human cytochromes P450. Drug Metab Dispos. 2002 Jul;30(7):805-13.

REF 144

The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist. J Pharmacol Exp Ther. 2001 Dec;299(3):883-93.

REF 145

The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J Psychopharmacol. 2005 Nov;19(6):609-13.

REF 146

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531)

REF 147

Simultaneous determination of nerisopam, a novel anxiolytic agent showing polymorphic metabolism, and its N-acetyl metabolite from human plasma by a validated high performance liquid chromatographic method. J Chromatogr B Biomed Appl. 1996 Mar 29;678(1):63-72.

REF 148

Synthesis and dual D2 and 5-HT1A receptor binding affinities of 7-piperazinyl and 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones. Med Chem. 2014;10(5):484-96.

REF 149

Effects of SUN 8399, a potent and selective 5-HT1A agonist, on conflict behavior and ambulatory activity in mice: comparison with those of buspirone, tandospirone and diazepam. Jpn J Pharmacol. 1994 Apr;64(4):273-80.

REF 150

Tolerance development to the vagal-mediated bradycardia produced by 5-HT1A receptor agonists. J Pharmacol Exp Ther. 1994 Nov;271(2):776-81.

REF 151

CN patent application no. 104151292, Indole derivative or a pharmaceutically acceptable salt thereof.

REF 152

Cardiovascular activity of A-74283, a 5-hydroxytryptamine 1A agent, in the spontaneously hypertensive rat. Pharmacology. 1998 Jan;56(1):17-29.

REF 153

Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.

REF 154

8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as busp... J Med Chem. 1996 Mar 1;39(5):1125-9.

REF 155

Quantitative determination of CGS 18102A, a new anxiolytic, in human plasma using capillary gas chromatography/mass spectrometry. Biomed Chromatogr. 1992 Sep-Oct;6(5):244-7.

REF 156

Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30.

REF 157

Neither in vivo MRI nor behavioural assessment indicate therapeutic efficacy for a novel 5HT1A agonist in rat models of ischaemic stroke. BMC Neuroscience 2009, 10:82.

REF 158

Pharmacological profile of (-)HT-90B, a novel 5-HT1A receptor agonist/5-HT2 receptor antagonist. Prog Neuropsychopharmacol Biol Psychiatry. 1995 Nov;19(7):1201-16.

REF 159

Chronic voluntary ethanol intake hypersensitizes 5-HT(1A) autoreceptors in C57BL/6J mice. J Neurochem. 2008 Dec;107(6):1660-70.

REF 160

Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity. J Pharmacol Exp Ther. 1994 Sep;270(3):1270-81.

REF 161

Influence of 5-HT1A receptor antagonism on plus-maze behaviour in mice. II. WAY 100635, SDZ 216-525 and NAN-190. Pharmacol Biochem Behav. 1997 Oct;58(2):593-603.

REF 162

Piperazinylalkyl heterocycles as potential antipsychotic agents. J Med Chem. 1995 Oct 13;38(21):4198-210.

REF 163

S 14506: novel receptor coupling at 5-HT(1A) receptors. Neuropharmacology. 2001 Mar;40(3):334-44.

REF 164

Development and validation of a capillary electrophoresis method for the enantiomeric purity determination of SLV307, a basic potential antipsychotic compound. Electrophoresis. 2004 Aug;25(16):2854-9.

REF 165

Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. Life Sci. 1997;60(9):653-65.

REF 166

Cocaine and serotonin: a role for the 5-HT(1A) receptor site in the mediation of cocaine stimulant effects. Behav Brain Res. 2001 Nov 29;126(1-2):127-33.

REF 167

Involvement of 5-hydroxytryptamine(1A) receptors in nicotine-induced tail tremor in rats. Eur J Pharmacol. 2000 Nov 10;408(1):19-23.

REF 168

Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. J Med Chem. 1993 Oct 15;36(21):3161-5.

REF 169

Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4.

REF 170

R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30.

REF 171

Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. Bioorg Med Chem. 2008 Jul 15;16(14):6675-81.

REF 172

The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. Psychopharmacology (Berl). 2001 Aug;157(1):111-4.

REF 173

5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80.

REF 174

Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. J Med Chem. 2010 Jun 24;53(12):4803-7.

REF 175

1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.

REF 176

5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. J Med Chem. 1986 Feb;29(2):194-9.

REF 177

Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7.

REF 178

Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7.

REF 179

Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. J Med Chem. 1989 May;32(5):1052-6.

REF 180

Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands. J Med Chem. 1991 Jun;34(6):1850-4.

REF 181

Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new ... J Med Chem. 1994 Aug 19;37(17):2754-60.

REF 182

Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6628-32.

REF 183

The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66.

REF 184

5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8.

REF 185

Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. J Med Chem. 2006 Nov 2;49(22):6607-13.

REF 186

Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands. J Med Chem. 2005 Jan 13;48(1):266-73.

REF 187

Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity. Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31.

REF 188

Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity, Bioorg. Med. Chem. Lett. 7(3):241-246 (1997).

REF 189

Novel aminoethylbiphenyls as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22.

REF 190

SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. Bioorg Med Chem. 2010 Mar 1;18(5):1958-67.

REF 191

4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists, Bioorg. Med. Chem. Lett. 7(13):1635-1638 (1997).

REF 192

A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem. 2003 Sep 11;46(19):4188-95.

REF 193

3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic a... J Med Chem. 1990 Aug;33(8):2087-93.

REF 194

New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates. Bioorg Med Chem Lett. 1998 Feb 3;8(3):295-300.

REF 195

6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. J Med Chem. 1992 Oct 30;35(22):3984-90.

REF 196

Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4.

REF 197

Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.

REF 198

Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.

REF 199

Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):682-8.

REF 200

Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.

REF 201

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.

REF 202

Ergolines as selective 5-HT1 agonists. J Med Chem. 1988 Aug;31(8):1512-9.

REF 203

SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.

REF 204

WO patent application no. 2012,0025,83, Method for treating schizophrenia and related diseases with a combination therapy.

REF 205

Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.

REF 206

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.

REF 207

Diagnosis of migraine with aura, depression and anxiety from allelic variations in dopaminergic genes

REF 208

Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in ... J Nat Prod. 2006 Mar;69(3):432-5.

REF 209

Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-... J Med Chem. 1985 Oct;28(10):1540-2.

REF 210

Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol. 1998 Aug 21;355(2-3):245-56.

REF 211

Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.

REF 212

3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem. 1999 Dec 2;42(24):4981-5001.

REF 213

Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21.

REF 214

Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor act... J Med Chem. 2008 Sep 25;51(18):5813-22.

REF 215

Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23.

REF 216

Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands. J Med Chem. 1988 Oct;31(10):1968-71.

REF 217

p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.

REF 218

A 18F-MPPF PET normative database of 5-HT1A receptor binding in men and women over aging. J Nucl Med. 2005 Dec;46(12):1980-9.

REF 219

New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. J Med Chem. 1996 Jan 5;39(1):176-82.

REF 220

Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46.

REF 221

Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804.

REF 222

Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.

REF 223

Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. J Pharmacol Exp Ther. 1998 Mar;284(3):1082-94.

REF 224

Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat. Neuropharmacology. 1998 Jun;37(6):769-80.

REF 225

SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol. 2001 Jul;133(6):797-806.

REF 226

Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80.

REF 227

Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43.

REF 228

Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor. Bioorg Med Chem Lett. 2005 Feb 1;15(3):747-50.

REF 229

Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione ... J Med Chem. 2005 Apr 21;48(8):3076-9.

REF 230

Effect of SR 59026A, a new 5-HT(1A) receptor agonist, on sexual activity in male rats. Behav Pharmacol. 1995 Apr;6(3):276-282.

REF 231

Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J Pharmacol Exp Ther. 1994 Nov;271(2):875-83.

REF 232

(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997).

REF 233

N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. J Med Chem. 1997 Apr 11;40(8):1252-7.

REF 234

Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.

REF 235

[11C]-WAY100635 PET demonstrates marked 5-HT1A receptor changes in sporadic ALS. Brain. 2005 Apr;128(Pt 4):896-905.

REF 236

Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem. 2000 Nov 30;43(24):4701-10.

REF 237

[(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. Naunyn Schmiedebergs Arch Pharmacol. 2010 Oct;382(4):321-30.

REF 238

Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep. 2004 Apr;24(2):101-15.

REF 239

Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. Eur J Pharmacol. 1998 Nov 6;360(2-3):219-25.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Yuzong CHEN

Prof. Feng ZHU