Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T78709 | ||||
Target Name | 5-HT 1A receptor (HTR1A) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Buspirone | Drug Info | IC50 = 24 nM | [62] | |
Adatanserin | Drug Info | Ki = 1 nM | [53] | ||
Bifeprunox | Drug Info | Ki = 64.6 nM | [59] | ||
BTS-79018 | Drug Info | Ki = 3.6 nM | [54] | ||
Flibanserin | Drug Info | Ki = 1 nM | |||
OPC-14523 | Drug Info | IC50 = 2.3 nM | [56] | ||
PD-158771 | Drug Info | Ki = 2.6 nM | [55] | ||
Sarizotan | Drug Info | Ki = 0.1 nM | [58] | ||
SLV-313 | Drug Info | Ki = 0.79 nM | [60] | ||
SSR-181507 | Drug Info | Ki = 0.242 nM | [57] | ||
Vilazodone | Drug Info | IC50 = 0.2 nM | [61] | ||
1192U90 | Drug Info | Ki = 3.8 nM | [63] | ||
(3-Chloro-phenyl)-piperazin-1-yl-methanone | Drug Info | Ki = 17100 nM | [38] | ||
(R)-(-)-10-methyl-11-hydroxyaporphine | Drug Info | Ki = 216 nM | [19] | ||
(R)-11-Amino-2-methoxyaporphine | Drug Info | Ki = 640 nM | [24] | ||
(R)-2,11-Diaminoaporphine | Drug Info | Ki = 2300 nM | [24] | ||
1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | Ki = 380 nM | [39] | ||
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane | Drug Info | Ki = 16 nM | [31] | ||
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane | Drug Info | Ki = 8 nM | [31] | ||
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane | Drug Info | Ki = 16 nM | [31] | ||
1,6-bis(4-m-tolylpiperazin-1-yl)hexane | Drug Info | Ki = 48 nM | [31] | ||
1,6-bis(4-phenylpiperazin-1-yl)hexane | Drug Info | Ki = 3 nM | [31] | ||
1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | Ki = 141 nM | [12] | ||
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | Ki = 680 nM | [38] | ||
1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | Ki = 1035 nM | [38] | ||
1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | Ki = 1020 nM | [40] | ||
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine | Drug Info | Ki = 116 nM | [28] | ||
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine | Drug Info | Ki = 4.5 nM | [29] | ||
1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | Ki = 31 nM | [28] | ||
1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | Ki = 9 nM | [28] | ||
1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | Ki = 8 nM | [28] | ||
1-(2-(benzyloxy)phenyl)piperazine | Drug Info | Ki = 28 nM | [28] | ||
1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | Ki = 189 nM | [28] | ||
1-(2-Butoxy-phenyl)-piperazine | Drug Info | Ki = 19.3 nM | [36] | ||
1-(2-Chloro-phenyl)-piperazine | Drug Info | Ki = 226 nM | [13] | ||
1-(2-Ethoxy-phenyl)-piperazine | Drug Info | Ki = 42.6 nM | [36] | ||
1-(2-Fluoro-phenyl)-piperazine | Drug Info | Ki = 57.9 nM | [36] | ||
1-(2-Isopropoxy-phenyl)-piperazine | Drug Info | Ki = 19 nM | [36] | ||
1-(2-Methoxy-phenyl)-4-propyl-piperazine | Drug Info | Ki = 249 nM | [44] | ||
1-(2-Methoxy-phenyl)-piperazine | Drug Info | Ki = 281 nM | [13] | ||
1-(2-methoxyphenyl)-4-pentylpiperazine | Drug Info | Ki = 5.16 nM | [33] | ||
1-(2-phenoxyphenyl)piperazine | Drug Info | Ki = 128 nM | [28] | ||
1-(3-Fluoro-phenyl)-piperazine | Drug Info | Ki = 86.5 nM | [36] | ||
1-(3-Nitro-phenyl)-piperazine | Drug Info | Ki = 250 nM | [36] | ||
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | Ki = 820 nM | [38] | ||
1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | Ki = 2.8 nM | [50] | ||
1-(benzyloxy)-2-(2-phenylethyl)benzene | Drug Info | Ki = 5000 nM | [17] | ||
1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene | Drug Info | Ki = 5000 nM | [17] | ||
1-Benzyl-4-chroman-2-ylmethyl-piperazine | Drug Info | Ki = 20.7 nM | [7] | ||
1-Butyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | Ki = 57 nM | [44] | ||
1-Ethyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | Ki = 203 nM | [44] | ||
1-Methyl-1,3-dihydro-indol-2-one | Drug Info | Ki = 29 nM | [2] | ||
1-Naphthalen-2-yl-piperazine | Drug Info | Ki = 265 nM | [39] | ||
1-naphthylpiperazine | Drug Info | Ki = 5 nM | [39] | ||
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | Ki = 351 nM | |||
1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene | Drug Info | Ki = 5000 nM | [17] | ||
2-(2'-methyl-biphenyl-3-yl)-ethylamine | Drug Info | Ki = 1470 nM | [18] | ||
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | Ki = 1710 nM | [40] | ||
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 16 nM | [29] | ||
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 13 nM | [29] | ||
2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | Ki = 3500 nM | [40] | ||
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 92 nM | [29] | ||
2-(3-Bromophenylthio)-N,N-dimethylethanamine | Drug Info | Ki = 676 nM | [30] | ||
2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | Ki = 2660 nM | [40] | ||
2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | Ki = 297 nM | [7] | ||
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | Ki = 2900 nM | [40] | ||
2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | Ki = 2830 nM | [40] | ||
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine | Drug Info | Ki = 613 nM | |||
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | IC50 = 86.4 nM | [4] | ||
2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine | Drug Info | Ki = 516 nM | [30] | ||
2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol | Drug Info | Ki = 2520 nM | |||
2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 101 nM | [29] | ||
2-Piperazin-1-yl-benzonitrile | Drug Info | Ki = 26.1 nM | [36] | ||
2-Piperazin-1-yl-phenol | Drug Info | Ki = 150 nM | [38] | ||
2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | Ki = 5000 nM | [17] | ||
3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole | Drug Info | IC50 = 140 nM | [34] | ||
3-(1-Propyl-pyrrolidin-3-yl)-phenol | Drug Info | Ki = 201 nM | |||
3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | IC50 = 19.6 nM | [4] | ||
3-(2-Benzylamino-ethoxy)-phenol | Drug Info | Ki = 1782 nM | [52] | ||
3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine | Drug Info | Ki = 807 nM | |||
3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | Ki = 260 nM | [7] | ||
3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one | Drug Info | Ki = 120 nM | [7] | ||
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | Ki = 60 nM | [29] | ||
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | Ki = 345 nM | [38] | ||
3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | IC50 = 420 nM | [5] | ||
3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | IC50 = 630 nM | [5] | ||
3-Naphthalen-1-yl-1-propyl-pyrrolidine | Drug Info | Ki = 73 nM | |||
3-Naphthalen-1-yl-pyrrolidine | Drug Info | Ki = 95 nM | |||
3-Phenyl-1-propyl-pyrrolidine | Drug Info | Ki = 453 nM | |||
3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | Ki = 5000 nM | [17] | ||
4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol | Drug Info | Ki = 1772 nM | [21] | ||
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | Ki = 57 nM | [28] | ||
4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | Ki = 47 nM | [28] | ||
4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | Ki = 5 nM | [28] | ||
4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 11 nM | [28] | ||
4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | Ki = 77 nM | [28] | ||
4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 117 nM | [28] | ||
4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | Ki = 606 nM | [28] | ||
4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | Ki = 364 nM | [28] | ||
4-(2-(benzyloxy)phenyl)piperidine | Drug Info | Ki = 121 nM | [28] | ||
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 4.6 nM | [29] | ||
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 21 nM | [28] | ||
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 156 nM | [28] | ||
4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | Ki = 128 nM | [28] | ||
4-(2-phenoxyphenyl)piperidine | Drug Info | Ki = 63 nM | [28] | ||
4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | Ki = 20 nM | [28] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki = 280 nM | [32] | ||
4-Benzyl-1-chroman-2-ylmethyl-piperidine | Drug Info | Ki = 11.5 nM | [7] | ||
4-Benzyl-1-chroman-3-ylmethyl-piperidine | Drug Info | Ki = 226 nM | [7] | ||
5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 1080 nM | [22] | ||
5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 1701 nM | [22] | ||
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 1081 nM | [22] | ||
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 192 nM | [22] | ||
8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine | Drug Info | Ki = 158 nM | |||
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | Ki = 1900 nM | [39] | ||
8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | Ki = 415 nM | [39] | ||
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 32 nM | [22] | ||
8-Methoxy-quinolin-2-ylamine | Drug Info | Ki = 10400 nM | [39] | ||
9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine | Drug Info | Ki = 2520 nM | |||
A-80426 | Drug Info | Ki = 2 nM | [11] | ||
AGROCLAVINE | Drug Info | IC50 = 140 nM | [35] | ||
AR-129330 | Drug Info | IC50 = 16.9 nM | [26] | ||
BMY-7378 | Drug Info | Ki = 8.2 nM | [47] | ||
BP-897 | Drug Info | Ki = 4.9 nM | [3] | ||
Brolamfetamine | Drug Info | Ki = 3340 nM | [40] | ||
CGS-12066B | Drug Info | IC50 = 19 nM | [34] | ||
CHLOROPHENYLPIPERAZINE | Drug Info | Ki = 25 nM | [36] | ||
CP-293019 | Drug Info | IC50 = 180 nM | [51] | ||
ESCHOLTZINE | Drug Info | Ki = 6000 nM | [14] | ||
Etisulergine | Drug Info | IC50 = 26 nM | [41] | ||
GR-127935 | Drug Info | IC50 = 425 nM | [1] | ||
LY-334370 | Drug Info | Ki = 22 nM | [6] | ||
LYSERGIC ACID DIETHYLAMIDE | Drug Info | Ki = 5.1 nM | [42] | ||
MAZAPERTINE | Drug Info | Ki = 1.7 nM | [43] | ||
MCL-516 | Drug Info | Ki = 151 nM | [24] | ||
N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine | Drug Info | Ki = 78.4 nM | [21] | ||
N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine | Drug Info | Ki = 233 nM | [21] | ||
N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide | Drug Info | Ki = 161 nM | [25] | ||
N-methyllaurotetanine | Drug Info | Ki = 85 nM | [14] | ||
N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide | Drug Info | Ki = 11 nM | [37] | ||
PB-28 | Drug Info | Ki = 28.6 nM | [46] | ||
PG-01037 | Drug Info | Ki = 85.4 nM | [20] | ||
PHENYLPIPERAZINE | Drug Info | Ki = 135 nM | [39] | ||
QUIPAZINE | Drug Info | Ki = 1584 nM | [27] | ||
RWJ-25730 | Drug Info | Ki = 3.3 nM | [43] | ||
SB-271046 | Drug Info | Ki = 340 nM | [23] | ||
SB-656104 | Drug Info | Ki = 562 nM | [9] | ||
SEROTONIN | Drug Info | Ki = 1.6 nM | [27] | ||
SNAP-8719 | Drug Info | Ki = 300 nM | [10] | ||
Sumanirole | Drug Info | Ki = 73 nM | [48] | ||
Sunepitron | Drug Info | Ki = 92 nM | [15] | ||
TERTATOLOL | Drug Info | Ki = 18.2 nM | |||
TFMPP | Drug Info | Ki = 20 nM | [38] | ||
TIOSPIRONE | Drug Info | IC50 = 2.85 nM | [16] | ||
UH-232 | Drug Info | Ki = 168 nM | |||
UH-301 | Drug Info | Ki = 52 nM | [49] | ||
WAY-466 | Drug Info | Ki = 234 nM | [8] | ||
WB-4101 | Drug Info | Ki = 2.68 nM | [45] | ||
[3H]spiperone | Drug Info | Ki = 602 nM | [45] | ||
References | |||||
REF 1 | New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenyl... J Med Chem. 2000 Feb 10;43(3):517-25. | ||||
REF 2 | 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 3 | Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of... J Med Chem. 2003 Aug 28;46(18):3822-39. | ||||
REF 4 | 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 5 | 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 6 | Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6011-6. | ||||
REF 7 | 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 8 | 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 9 | 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 10 | 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 11 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | ||||
REF 12 | 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 13 | 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 14 | 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 15 | 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 16 | Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. J Med Chem. 1991 Nov;34(11):3316-28. | ||||
REF 17 | Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. J Med Chem. 2006 Nov 2;49(22):6607-13. | ||||
REF 18 | Novel aminoethylbiphenyls as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22. | ||||
REF 19 | 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 20 | 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 21 | Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. | ||||
REF 22 | 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 23 | 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 24 | Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. Bioorg Med Chem. 2008 Jul 15;16(14):6675-81. | ||||
REF 25 | 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 26 | Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. | ||||
REF 27 | 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 28 | 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 29 | 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 30 | SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. | ||||
REF 31 | 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 32 | 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 33 | 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 34 | 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 35 | Ergolines as selective 5-HT1 agonists. J Med Chem. 1988 Aug;31(8):1512-9. | ||||
REF 36 | 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 37 | Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands. J Med Chem. 1988 Oct;31(10):1968-71. | ||||
REF 38 | Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4. | ||||
REF 39 | 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80. | ||||
REF 40 | 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 41 | 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 42 | 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 43 | 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 44 | 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 45 | 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 46 | 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 47 | 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 48 | Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites. J Med Chem. 1997 Feb 28;40(5):639-46. | ||||
REF 49 | 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 50 | 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8. | ||||
REF 51 | 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 52 | 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 53 | 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 54 | N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. J Med Chem. 1999 Aug 26;42(17):3342-55. | ||||
REF 55 | PD 158771, a potential antipsychotic agent with D(2)/D(3) partial agonist and 5-HT(1A) agonist actions. I. Neurochemical effects. Neuropharmacology. 2000 Apr 27;39(7):1197-210. | ||||
REF 56 | Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88. | ||||
REF 57 | SSR181507, a dopamine D(2) receptor antagonist and 5-HT(1A) receptor agonist. I: Neurochemical and electrophysiological profile. Neuropsychopharmacology. 2003 Dec;28(12):2064-76. | ||||
REF 58 | Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile. J Neural Transm (Vienna). 2004 Feb;111(2):113-26. | ||||
REF 59 | Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatm... Int J Neuropsychopharmacol. 2005 Sep;8(3):341-56. | ||||
REF 60 | SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 recept... Neuropsychopharmacology. 2007 Jan;32(1):78-94. | ||||
REF 61 | 5-HT1 receptor augmentation strategies as enhanced efficacy: therapeutics for psychiatric disorders. Curr Top Med Chem. 2008;8(12):1008-23. | ||||
REF 62 | Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors. Biol Psychiatry. 1985 Sep;20(9):971-9. | ||||
REF 63 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. J Med Chem. 1996 Nov 22;39(24):4692-703. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.