Target Information

Target General Information

Target ID

T11072 (Former ID: TTDS00100)

Target Name

5-HT 1D receptor (HTR1D)

Synonyms

Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D

Gene Name

HTR1D

Target Type

Successful target

[1]

Disease

[+] 2 Target-related Diseases

Migraine [ICD-11: 8A80]

Pituitary gland disorder [ICD-11: 5A60-5A61]

Function

Functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other 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. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).

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BioChemical Class

GPCR rhodopsin

UniProt ID

5HT1D_HUMAN

Sequence

MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT
CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK
AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT
TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT
KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN
EEFRQAFQKIVPFRKAS

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 7 Approved Drugs

Almogran

Drug Info

Approved

Migraine

[2]

Eletriptan

Drug Info

Approved

Migraine

[3], [4]

Frovatriptan

Drug Info

Approved

Migraine

[4], [5]

Metergolin

Drug Info

Approved

Hyperprolactinaemia

[6]

Rizatriptan

Drug Info

Approved

Migraine

[7]

Sumatriptan

Drug Info

Approved

Migraine

[4], [8]

Zolmitriptan

Drug Info

Approved

Migraine

[9], [10]

Clinical Trial Drug(s)

[+] 4 Clinical Trial Drugs

Neu-P11

Drug Info

Phase 2

Insomnia

[11]

NXN-188

Drug Info

Phase 2

Migraine

[12]

TGBA01AD

Drug Info

Phase 2

Mood disorder

[13]

Tonabersat

Drug Info

Phase 2

Epilepsy

[14]

Discontinued Drug(s)

[+] 14 Discontinued Drugs

Alniditan

Drug Info

Discontinued in Phase 3

Migraine

[15], [16]

Avitriptan

Drug Info

Discontinued in Phase 3

Migraine

[17]

BMS-181101

Drug Info

Discontinued in Phase 2

Mood disorder

[18], [19]

CP-122288

Drug Info

Discontinued in Phase 2

Migraine

[20], [21]

Elzasonan hydrochloride

Drug Info

Discontinued in Phase 2

Mood disorder

[13]

IS-159

Drug Info

Discontinued in Phase 2

Migraine

[22]

PNU-142633

Drug Info

Discontinued in Phase 2

Migraine

[23]

ALX-0646

Drug Info

Discontinued in Phase 1

Migraine

[24]

Tidembersat

Drug Info

Discontinued in Phase 1

Migraine

[25]

BMS-181885

Drug Info

Terminated

Migraine

[28]

GR-127935

Drug Info

Terminated

Major depressive disorder

[29], [30]

L-694247

Drug Info

Terminated

Migraine

[31], [32]

PNU-109291

Drug Info

Terminated

Migraine

[33], [34]

VR-147

Drug Info

Terminated

Migraine

[35]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

Donitriptan

Drug Info

Preclinical

Migraine

[26], [27]

Mode of Action

[+] 4 Modes of Action

Agonist

[+] 32 Agonist drugs

Almogran

Drug Info

[36]

Rizatriptan

Drug Info

[39]

Sumatriptan

Drug Info

[1], [40], [41], [42], [43]

FKB01MD

Drug Info

[44]

Neu-P11

Drug Info

[45]

Tonabersat

Drug Info

[48], [49]

Alniditan

Drug Info

[50], [49], [50]

Avitriptan

Drug Info

[51], [49]

CP-122288

Drug Info

[53], [49]

PNU-142633

Drug Info

[56], [49]

ALX-0646

Drug Info

[49]

BMS-181885

Drug Info

[52], [49]

L-694247

Drug Info

[59], [49]

PNU-109291

Drug Info

[62], [49]

1-naphthylpiperazine

Drug Info

[72], [66]

2-methyl-5-HT

Drug Info

[76]

5-CT

Drug Info

[38]

7-methoxy-1-naphthylpiperazine

Drug Info

[71]

alpha-methyl-5-HT

Drug Info

[76]

BRL-15572

Drug Info

[81]

dipropyl-5-CT

Drug Info

[72]

EDMT

Drug Info

[82]

lysergic acid

Drug Info

[76]

lysergol

Drug Info

[72]

SB 216641

Drug Info

[81]

TFMPP

Drug Info

[38], [65]

[125I]GTI

Drug Info

[89]

[3H]5-CT

Drug Info

[90]

[3H]5-HT

Drug Info

[50]

[3H]8-OH-DPAT

Drug Info

[91]

[3H]eletriptan

Drug Info

[92]

[3H]sumatriptan

Drug Info

[92]

Modulator

[+] 10 Modulator drugs

Eletriptan

Drug Info

[37]

Frovatriptan

Drug Info

[37]

Zolmitriptan

Drug Info

[37]

NXN-188

Drug Info

[46]

TGBA01AD

Drug Info

[47]

Elzasonan hydrochloride

Drug Info

[54]

IS-159

Drug Info

[55]

Donitriptan

Drug Info

[57]

GR-127935

Drug Info

[58]

VR-147

Drug Info

[63], [49]

Antagonist

[+] 12 Antagonist drugs

Metergolin

Drug Info

[38]

BMS-181101

Drug Info

[52], [49]

Tidembersat

Drug Info

[49]

9-OH-risperidone

Drug Info

[79]

bufotenine

Drug Info

[76]

L-772,405

Drug Info

[85]

m-chlorophenylpiperazine

Drug Info

[38]

MPDT

Drug Info

[82]

SB 272183

Drug Info

[86]

SB 649915

Drug Info

[87]

SB 714786

Drug Info

[87]

[3H]GR 125,743

Drug Info

[90]

Inhibitor

[+] 53 Inhibitor drugs

L-741604

Drug Info

[60]

L-775606

Drug Info

[61]

(+/-)-nantenine

Drug Info

[64]

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

Drug Info

[65]

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

Drug Info

[66]

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

Drug Info

[67]

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

Drug Info

[65]

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

Drug Info

[65]

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

Drug Info

[68]

1-(2-Butoxy-phenyl)-piperazine

Drug Info

[69]

1-(2-Ethoxy-phenyl)-piperazine

Drug Info

[69]

1-(2-Fluoro-phenyl)-piperazine

Drug Info

[69]

1-(2-Isopropoxy-phenyl)-piperazine

Drug Info

[69]

1-(2-Methoxy-phenyl)-piperazine

Drug Info

[69]

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

Drug Info

[70]

1-(3-Fluoro-phenyl)-piperazine

Drug Info

[69]

1-(3-Nitro-phenyl)-piperazine

Drug Info

[69]

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

Drug Info

[65]

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

Drug Info

[71]

1-Naphthalen-2-yl-piperazine

Drug Info

[66]

2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole

Drug Info

[73]

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

Drug Info

[68]

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

Drug Info

[68]

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

Drug Info

[68]

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

Drug Info

[68]

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

Drug Info

[68]

2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole

Drug Info

[73]

2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine

Drug Info

[74]

2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine

Drug Info

[75]

2-Piperazin-1-yl-benzonitrile

Drug Info

[69]

2-Piperazin-1-yl-phenol

Drug Info

[65]

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

Drug Info

[65]

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

Drug Info

[77]

5-amino-3-(N-methylpiperidin-4-yl)-1H-indole

Drug Info

[61]

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

Drug Info

[77]

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

Drug Info

[77]

5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole

Drug Info

[78]

5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole

Drug Info

[78]

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

Drug Info

[66]

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

Drug Info

[66]

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

Drug Info

[77]

8-Methoxy-quinolin-2-ylamine

Drug Info

[66]

AGROCLAVINE

Drug Info

[80]

Brolamfetamine

Drug Info

[68]

CHLOROPHENYLPIPERAZINE

Drug Info

[69]

Etisulergine

Drug Info

[83]

L-747201

Drug Info

[84]

L-760790

Drug Info

[60]

PHENYLPIPERAZINE

Drug Info

[66]

QUIPAZINE

Drug Info

[66]

SEROTONIN

Drug Info

[61]

WAY-466

Drug Info

[88]

[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine

Drug Info

[78]

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 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

[+] 5 WikiPathways

Serotonin HTR1 Group and FOS Pathway

Monoamine GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.

REF 2

Drug information of Almogran, 2008. eduDrugs.

REF 3

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: 40).

REF 4

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 5

REF 6

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

REF 7

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

REF 8

REF 9

REF 10

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020768.

REF 11

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 12

ClinicalTrials.gov (NCT00920686) Study of NXN 188 for the Treatment of Migraine With Aura. U.S. National Institutes of Health.

REF 13

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

REF 14

ClinicalTrials.gov (NCT00534560) Dose Ranging Study of the Efficacy and Tolerability of Tonabersat in the Prophylaxis of Migraine Headache. U.S. National Institutes of Health.

REF 15

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006286)

REF 17

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002927)

REF 18

REF 19

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005177)

REF 20

REF 21

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005787)

REF 22

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005786)

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 800013927)

REF 24

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008400)

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010348)

REF 26

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012002)

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007062)

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 800002743)

REF 31

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003457)

REF 33

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010481)

REF 35

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023937)

REF 36

Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75.

REF 37

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

REF 38

Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.

REF 39

An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.

REF 40

5-Hydroxytryptamine(1F) receptors do not participate in vasoconstriction: lack of vasoconstriction to LY344864, a selective serotonin(1F) receptor agonist in rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):935-9.

REF 41

5-Hydroxytryptamine receptor agonists for the abortive treatment of vascular headaches block mast cell, endothelial and platelet activation within the rat dura mater after trigeminal stimulation. Brain Res. 1992 Jun 26;583(1-2):137-49.

REF 42

Novel approaches to the treatment of nausea and vomiting. Dig Dis. 1999;17(3):125-32.

REF 43

Serotonin in migraine: theories, animal models and emerging therapies. Prog Drug Res. 1998;51:219-44.

REF 44

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

REF 45

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

REF 46

Company report (NeurAxon)

REF 47

Company report (Fabrekramer)

REF 48

The potential anti-migraine compound SB-220453 does not contract human isolated blood vessels or myocardium; a comparison with sumatriptan. Cephalalgia. 2000 Jul;20(6):538-45.

REF 49

Sustained pain relief with dihydroergotamine in migraine is potentially due to persistent binding to 5-HT1B and 5-HT1D receptors. . The Journal of Headache and Pain 201314(Suppl 1):P75.

REF 50

Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65.

REF 51

Safety trial with the 5HT1B/1D agonist avitriptan (BMS-180048) in patients with migraine who have experienced pressure, tightness, and/or pain in the chest, neck, and/or throat following sumatriptan.Cephalalgia. 1998 Oct;18(8):546-51.

REF 52

Sensitive triple-quadrupole mass spectrometric assay for the determination of BMS-181885, a 5-HT1 agonist, in human plasma following solid phase extraction. Biomed Chromatogr. 1999 Oct;13(6):425-30.

REF 53

The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater. Neuropharmacology. 1997 Jan;36(1):83-91.

REF 54

DOI: 10.1002/9781118541203.xen439

REF 55

Pronounced effect of caprylocaproyl macrogolglycerides on nasal absorption of IS-159, a peptide serotonin 1B/1D-receptor agonist. Clin Pharmacol Ther. 2000 Aug;68(2):114-21.

REF 56

Further characterization of the 5-HT1 receptors mediating cardiac sympatho-inhibition in pithed rats: pharmacological correlation with the 5-HT1B a... Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):220-7.

REF 57

Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors.Br J Pharmacol.2006 Sep;149(1):82-91.

REF 58

GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61.

REF 59

L-694,247: a potent 5-HT1D receptor agonist. Br J Pharmacol. 1993 Nov;110(3):1196-200.

REF 60

3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1999 Feb 25;42(4):691-705.

REF 61

Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-pip... J Med Chem. 2008 Jun 26;51(12):3609-16.

REF 62

Role of 5-HT(1) receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn. Br J Pharmacol. 2012 Mar;165(6):1956-65.

REF 63

US patent application no. 2010,0112,050, Dosage form for insertion into the mouth.

REF 64

Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.

REF 65

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

REF 66

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

REF 67

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 68

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 69

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 70

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

REF 71

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

REF 72

Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4.

REF 73

2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4697-9.

REF 74

5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. J Med Chem. 1994 Sep 2;37(18):2828-30.

REF 75

5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine. Bioorg Med Chem Lett. 2000 May 1;10(9):903-5.

REF 76

Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Mol Pharmacol. 1996 Dec;50(6):1567-80.

REF 77

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 78

5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists. Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.

REF 79

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 80

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

REF 81

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 82

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

REF 83

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 84

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1997 Oct 24;40(22):3501-3.

REF 85

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 86

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 87

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

REF 88

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 89

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