Target General Infomation
Target ID
T16691 (Former ID: TTDC00185)
Target Name
5-HT 6 receptor (HTR6)
Synonyms
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
Gene Name
HTR6
Target Type
Clinical trial target
[1]
Disease [+] 2 Target-related Diseases +
1 Alzheimer disease [ICD-11: 8A20]
2 Schizophrenia [ICD-11: 6A20]
Function
The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs. Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity. Is an activator of TOR signaling. This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen.
BioChemical Class
GPCR rhodopsin
UniProt ID
5HT6R_HUMAN
Sequence
MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
FNIDPAEPELRPHPLGIPTN
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 13 Clinical Trial Drugs +
1 LU AE58054 Drug Info Phase 3 Schizophrenia [2], [3]
2 SB-742457 Drug Info Phase 3 Alzheimer disease [4]
3 AVN 211 Drug Info Phase 2/3 Schizophrenia [5]
4 AVN 101 Drug Info Phase 2 Anxiety disorder [6]
5 AVN 322 Drug Info Phase 2 Cognitive impairment [7]
6 PF-05212377 Drug Info Phase 2 Alzheimer disease [8]
7 SAM-531 Drug Info Phase 2 Alzheimer disease [9], [10]
8 SUVN-502 Drug Info Phase 2 Neurological disorder [11]
9 SYN-120 Drug Info Phase 2 Alzheimer disease [12]
10 11C-GSK-215083 Drug Info Phase 1 Neurodegenerative disorder [13], [14]
11 ABT-354 Drug Info Phase 1 Alzheimer disease [15]
12 BVT-74316 Drug Info Phase 1 Obesity [16]
13 PRX-07034 Drug Info Phase 1 Obesity [17]
Patented Agent(s) [+] 2 Patented Agents +
1 PMID30124346-Compound-13TABLE4 Drug Info Patented Attention deficit hyperactivity disorder [18]
2 PMID30124346-Compound-34TABLE4 Drug Info Patented Attention deficit hyperactivity disorder [18]
Discontinued Drug(s) [+] 3 Discontinued Drugs +
1 AVN 397 Drug Info Discontinued in Phase 2 Anxiety disorder [19]
2 SYN-114 Drug Info Discontinued in Phase 1 Cognitive impairment [20]
3 WAY-181187 Drug Info Discontinued in Phase 1 Anxiety disorder [21], [22]
Mode of Action [+] 6 Modes of Action +
Enhancer [+] 1 Enhancer drugs +
1 LU AE58054 Drug Info [23]
Antagonist [+] 24 Antagonist drugs +
1 SB-742457 Drug Info [24], [25]
2 PF-05212377 Drug Info [27]
3 SAM-531 Drug Info [28]
4 SUVN-502 Drug Info [29]
5 SYN-120 Drug Info [30]
6 11C-GSK-215083 Drug Info [31]
7 BVT-74316 Drug Info [33]
8 PRX-07034 Drug Info [34]
9 AVN 397 Drug Info [26]
10 SYN-114 Drug Info [35]
11 2-bromo-LSD Drug Info [44]
12 5-HT 6 antagonists Drug Info [62]
13 5-HT 6 receptor antagonists Drug Info [62]
14 alpha-ergocryptine Drug Info [66]
15 bufotenine Drug Info [53]
16 fluperlapine Drug Info [71]
17 MPDT Drug Info [70]
18 SB 258585 Drug Info [73]
19 SB399885 Drug Info [76]
20 SUVN-501 Drug Info [62]
21 SUVN-504 Drug Info [62]
22 SUVN-507 Drug Info [62]
23 [125I]SB-258585 Drug Info [73]
24 [3H]Ro 63-0563 Drug Info [1], [75]
Modulator [+] 8 Modulator drugs +
1 AVN 211 Drug Info [26]
2 AVN 101 Drug Info [26]
3 ABT-354 Drug Info [32]
4 AVN 322 Drug Info [24]
5 WAY-181187 Drug Info [36]
6 AMR-SIX-1 Drug Info [62]
7 SB-214111 Drug Info [74]
8 SEL-73 Drug Info [62]
Ligand [+] 2 Ligand drugs +
1 PMID30124346-Compound-13TABLE4 Drug Info [18]
2 PMID30124346-Compound-34TABLE4 Drug Info [18]
Inhibitor [+] 76 Inhibitor drugs +
1 (+/-)-nantenine Drug Info [37]
2 1-(2-Methoxy-phenyl)-piperazine Drug Info [38]
3 1-(3-(benzyloxy)-2-methylphenyl)piperazine Drug Info [39]
4 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [40]
5 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole Drug Info [41]
6 1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole Drug Info [42]
7 1-Benzenesulfonyl-3-piperidin-4-yl-1H-indole Drug Info [43]
8 1-phenylthio-N,N-dimethyltryptamine Drug Info [45]
9 2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine Drug Info [46]
10 2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine Drug Info [47]
11 2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine Drug Info [47]
12 2-(1-tosyl-1H-indol-3-yl)ethanamine Drug Info [46]
13 2-(1H-indol-3-yl)-N,N-dimethylethanamine Drug Info [48]
14 2-(3-(phenylsulfonyl)-1H-indol-1-yl)ethanamine Drug Info [49]
15 2-(3-benzenesulfonyl)phenyl-1-aminoethane Drug Info [50]
16 2-(3-phenylthio)phenyl)-1-aminoethane Drug Info [50]
17 2-(4-(benzenesulfonyl)phenyl)-1-aminoethane Drug Info [50]
18 2-Benzyl-4-piperazin-1-yl-1H-benzimidazole Drug Info [51]
19 2-Ethyl-5-methoxy-3-piperidin-4-yl-1H-indole Drug Info [52]
20 3-(2-Amino-ethyl)-2-methyl-1H-indol-5-ol Drug Info [54]
21 3-(phenylsulfonyl)-1-(piperidin-3-yl)-1H-indole Drug Info [55]
22 3-(phenylsulfonyl)-1-(piperidin-4-yl)-1H-indole Drug Info [55]
23 3-(phenylsulfonyl)-1-(pyrrolidin-3-yl)-1H-indole Drug Info [55]
24 4-((1H-indol-1-yl)methyl)benzenamine Drug Info [56]
25 4-(1H-Inden-1-ylmethyl)-phenylamine Drug Info [57]
26 4-(1H-indol-1-ylsulfonyl)benzenamine Drug Info [41]
27 4-(1H-Indol-3-ylmethyl)-phenylamine Drug Info [57]
28 4-(2-benzenesulfonylphenyl)piperazine Drug Info [50]
29 4-(3-benzenesulfonamidophenyl)piperazine Drug Info [50]
30 4-(3-benzenesulfonylphenyl)piperazine Drug Info [50]
31 4-(3-Methyl-indole-1-sulfonyl)-phenylamine Drug Info [38]
32 4-(3H-Inden-1-ylmethyl)-phenylamine Drug Info [57]
33 4-(4,6-dinitro-1H-indol-1-ylsulfonyl)benzenamine Drug Info [41]
34 4-(4-benzenesulfonamidophenyl)piperazine Drug Info [50]
35 4-(4-benzenesulfonylphenyl)piperazine Drug Info [50]
36 4-(4-methoxy-1H-indol-1-ylsulfonyl)benzenamine Drug Info [58]
37 4-(6-methoxy-1H-indol-1-ylsulfonyl)benzenamine Drug Info [58]
38 4-(Indan-1-ylsulfanyl)-phenylamine Drug Info [57]
39 4-(Indane-1-sulfonyl)-phenylamine Drug Info [57]
40 4-(Naphthalene-1-sulfonyl)-phenylamine Drug Info [38]
41 4-(piperazin-1-yl)-1H-indole Drug Info [41]
42 4-(piperazin-1-yl)-3-tosyl-1H-indazole Drug Info [59]
43 4-Indan-1-ylmethyl-phenylamine Drug Info [57]
44 4-Inden-(1E)-ylidenemethyl-phenylamine Drug Info [57]
45 5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [60]
46 5-(4-Methylpiperazin-1-yl)-3-tosyl-1H-indazole Drug Info [59]
47 5-MEO-DMT Drug Info [63]
48 5-METHOXYTRYPTAMINE Drug Info [64]
49 6-(piperazin-1-yl)-3-tosyl-1H-indazole Drug Info [59]
50 6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole Drug Info [65]
51 CHLOROPHENYLPIPERAZINE Drug Info [54]
52 DIMEBOLIN Drug Info [68]
53 E-6837 Drug Info [47]
54 EDMT Drug Info [47], [70]
55 METHIOTHEPIN Drug Info [72]
56 N,N-diethyl-2-(1H-indol-3-yl)ethanamine Drug Info [63]
57 N,N-dimethyl-2-(1-tosyl-1H-indol-3-yl)ethanamine Drug Info [56]
58 N-(3-(2-aminoethyl)phenyl)benzenesulfonamide Drug Info [50]
59 N-(3-(3-aminopropyl)phenyl)benzenesulfonamide Drug Info [50]
60 N-(3-(aminomethyl)phenyl)benzenesulfonamide Drug Info [50]
61 N-(3-aminophenyl)benzenesulfonamide Drug Info [50]
62 N-(4-(2-aminoethyl)phenyl)benzenesulfonamide Drug Info [50]
63 N-phenyl-3-(2-aminoethyl)benzenesulfonamide Drug Info [50]
64 OCTOCLOTHEPIN Drug Info [64]
65 QUIPAZINE Drug Info [54]
66 Ro-04-6790 Drug Info [47]
67 SB-271046 Drug Info [39]
68 SB-357134 Drug Info [75]
69 SEROTONIN Drug Info [72]
70 WAY-208466 Drug Info [49]
71 WAY-466 Drug Info [77]
72 [2-(3-Benzyl-3H-inden-1-yl)-ethyl]-methyl-amine Drug Info [57]
73 [2-(3-Benzyl-3H-indol-1-yl)-ethyl]-dimethyl-amine Drug Info [78]
74 [2-(3-Benzyl-indol-1-yl)-ethyl]-dimethyl-amine Drug Info [57]
75 [2-(3H-Indol-1-yl)-ethyl]-dimethyl-amine Drug Info [78]
76 [3H]spiperone Drug Info [54]
Agonist [+] 15 Agonist drugs +
1 1-naphthylpiperazine Drug Info [38], [44]
2 2-methyl-5-HT Drug Info [53]
3 5-CT Drug Info [61]
4 alpha-methyl-5-HT Drug Info [66]
5 BRL-15572 Drug Info [67]
6 DM-1451 Drug Info [69]
7 E6801 Drug Info [64]
8 EMD-386088 Drug Info [52]
9 lergotrile Drug Info [44]
10 LY 165,163 Drug Info [44]
11 m-chlorophenylpiperazine Drug Info [44]
12 OPC 4392 Drug Info [69]
13 TFMPP Drug Info [44]
14 [3H]5-CT Drug Info [62]
15 [3H]LSD Drug Info [69]
Target Regulators
Target-interacting Proteins
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 4 KEGG Pathways +
1 Calcium signaling pathway
2 cAMP signaling pathway
3 Neuroactive ligand-receptor interaction
4 Serotonergic synapse
Panther Pathway [+] 1 Panther Pathways +
1 Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Pathwhiz Pathway [+] 1 Pathwhiz Pathways +
1 Excitatory Neural Signalling Through 5-HTR 6 and Serotonin
Reactome [+] 2 Reactome Pathways +
1 Serotonin receptors
2 G alpha (s) signalling events
WikiPathways [+] 5 WikiPathways +
1 Serotonin Receptor 4/6/7 and NR3C Signaling
2 Monoamine GPCRs
3 GPCRs, Class A Rhodopsin-like
4 GPCR ligand binding
5 GPCR downstream signaling
Target-Related Models and Studies
Target Validation
Target QSAR Model
References
REF 1 The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. Mol Pharmacol. 1998 Sep;54(3):577-83.
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: 8689).
REF 3 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019915)
REF 4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 6 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030006)
REF 7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 8 ClinicalTrials.gov (NCT01712074) Study Evaluating TheSafety And Efficacy Of PF-05212377 Or Placebo In Subjects With Alzheimer's Disease With Existing Neuropsychiatric Symptoms On Donepezil. U.S. National Institutes of Health.
REF 9 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: 7356).
REF 10 ClinicalTrials.gov (NCT00895895) Study Comparing 3 Dosage Levels Of SAM-531 In Outpatients With Mild To Moderate Alzheimer Disease. U.S. National Institutes of Health.
REF 11 Clinical pipeline report, company report or official report of Suven Life Sciences.
REF 12 ClinicalTrials.gov (NCT02258152) SYN120 a Dual 5-HT6/5-HT2A Antagonist Proof of Concept Study to Evaluate Its Safety, Tolerability and Efficacy in Parkinson's Disease Dementia (SYNAPSE). U.S. National Institutes of Health.
REF 13 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: 8430).
REF 14 List of drugs in development for neurodegenerative diseases: update October 2011. Neurodegener Dis. 2012;9(4):210-83.
REF 15 ClinicalTrials.gov (NCT01908010) Safety, Tolerability, and Pharmacokinetics of ABT-354 in Subjects With Mild-to-Moderate Alzheimer's Disease on Stable Doses of Acetylcholinesterase Inhibitors. U.S. National Institutes of Health.
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 800023034)
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 800021329)
REF 18 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
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 800031584)
REF 20 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025583)
REF 21 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: 3240).
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 800021227)
REF 23 Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.
REF 24 5-HT6 receptors and Alzheimer's disease. Alzheimers Res Ther. 2013; 5(2): 15.
REF 25 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 26 Latrepirdine, a potential novel treatment for Alzheimer's disease and Huntington's chorea. Curr Opin Investig Drugs. 2010 January; 11(1): 80-91.
REF 27 PF-05212377 Alzheimer's Disease (Phase 2). Pfizer.
REF 28 Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9.
REF 29 Novel and Potent 5-Piperazinyl Methyl-N1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands. ACS Med Chem Lett. 2010 October 14; 1(7): 340-344.
REF 30 The Serotonin-6 Receptor as a Novel Therapeutic Target. Exp Neurobiol. 2011 December; 20(4): 159-168.
REF 31 Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor. J Nucl Med. 2012 Feb;53(2):295-303.
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 800035134)
REF 33 Pharmacological targeting of the serotonergic system for the treatment of obesity. J Physiol. 2009 January 1; 587(Pt 1): 49-60.
REF 34 Low-dose prazosin in combination with 5-HT6 antagonist PRX-07034 has antipsychotic effects. Can J Physiol Pharmacol. 2015 Jan;93(1):13-21.
REF 35 Lewy bodies. Proc Natl Acad Sci U S A. 2006 February 7; 103(6): 1661-1668.
REF 36 Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466.Neuropsychopharmacology.2008 May;33(6):1323-35.
REF 37 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 38 1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1707-11.
REF 39 Synthesis and SAR of tolylamine 5-HT6 antagonists. Bioorg Med Chem Lett. 2009 May 1;19(9):2409-12.
REF 40 The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66.
REF 41 Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5298-302.
REF 42 Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4780-5.
REF 43 N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2005 Jan 17;15(2):379-83.
REF 44 Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol. 1993 Mar;43(3):320-7.
REF 45 Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. J Med Chem. 2008 Feb 14;51(3):603-11.
REF 46 Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist. J Med Chem. 2007 Nov 15;50(23):5535-8.
REF 47 Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. J Med Chem. 2009 Feb 12;52(3):675-87.
REF 48 Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects. Arch Gen Psychiatry. 1994 Feb;51(2):85-97.
REF 49 Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. Bioorg Med Chem. 2009 Jul 15;17(14):5153-63.
REF 50 Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. J Med Chem. 2006 Aug 24;49(17):5217-25.
REF 51 Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation. J Med Chem. 2010 Feb 11;53(3):1357-69.
REF 52 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4.
REF 53 Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells. Neuropharmacology. 1997 Apr-May;36(4-5):713-20.
REF 54 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
REF 55 3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1657-60.
REF 56 Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1691-4.
REF 57 Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1987-91.
REF 58 Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3793-6.
REF 59 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. J Med Chem. 2010 Nov 11;53(21):7639-46.
REF 60 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 61 Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem. 1996 Jan;66(1):47-56.
REF 62 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. (Target id: 11).
REF 63 Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5832-5.
REF 64 Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J Med Chem. 2005 Mar 24;48(6):1781-95.
REF 65 A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3929-31.
REF 66 Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor. J Neurochem. 1998 Nov;71(5):2169-77.
REF 67 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 68 8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. Eur J Med Chem. 2010 Feb;45(2):782-9.
REF 69 Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology. 1999 Jun;20(6):612-27.
REF 70 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 71 Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.
REF 72 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. J Med Chem. 2010 Mar 25;53(6):2521-7.
REF 73 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585. Synapse. 2002 Sep 1;45(3):191-9.
REF 74 The distribution of 5-HT(6) receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT(6) receptor antagonist [(125)I]S... Brain Res. 2002 Apr 26;934(1):49-57.
REF 75 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 76 SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition ... Eur J Pharmacol. 2006 Dec 28;553(1-3):109-19.
REF 77 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 78 Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4569-73.

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