Target Information
Target General Infomation | |||||
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Target ID |
T16691
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Former ID |
TTDC00185
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Target Name |
5-hydroxytryptamine 6 receptor
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Gene Name |
HTR6
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Synonyms |
5-HT-6; 5-HT6 receptor; Serotonin receptor; Serotonin receptor 6; HTR6
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Target Type |
Clinical Trial
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Disease | Alzheimer disease; Anxiety disorder [ICD9:331, 300, 311; ICD10: G30, F32, F40-F42] | ||||
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
Alzheimer disease; Dementia [ICD9: 290-294, 331.0; ICD10: F01-F07, G30] | |||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3] | |||||
Emesis [ICD9: 787; ICD10: R11] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Neurodegenerative disease [ICD9: 330-337; ICD10: G30-G32] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
Unspecified [ICD code not available] | |||||
Function |
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. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity (By similarity). Is an activator of TOR signaling (PubMed:23027611).
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T16691
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UniProt ID | |||||
Sequence |
MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF FNIDPAEPELRPHPLGIPTN |
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Drugs and Mode of Action | |||||
Drug(s) | LU AE58054 | Drug Info | Phase 3 | Schizophrenia | [543246], [547850] |
AVN 101 | Drug Info | Phase 2 | Alzheimer disease; Anxiety disorder | [548893] | |
AVN 211 | Drug Info | Phase 2 | Schizophrenia | [548881] | |
PF-05212377 | Drug Info | Phase 2 | Alzheimer disease | [524103] | |
SAM-531 | Drug Info | Phase 2 | Alzheimer disease | [522658], [542377] | |
SB-742457 | Drug Info | Phase 2 | Alzheimer disease; Dementia | [547877] | |
SUVN-502 | Drug Info | Phase 2 | Neurological disease | [551708] | |
SYN-120 | Drug Info | Phase 2 | Alzheimer disease | [524945] | |
11C-GSK-215083 | Drug Info | Phase 1 | Neurodegenerative disease | [525385], [543132] | |
ABT-354 | Drug Info | Phase 1 | Alzheimer disease | [524382] | |
AVN 322 | Drug Info | Phase 1 | Alzheimer disease | [549023] | |
BVT-74316 | Drug Info | Phase 1 | Obesity | [548202] | |
PRX-07034 | Drug Info | Phase 1 | Obesity | [548037] | |
AVN 397 | Drug Info | Discontinued in Phase 2 | Alzheimer disease; Anxiety disorder | [549022] | |
SYN-114 | Drug Info | Discontinued in Phase 1 | Cognitive disorders | [548444] | |
WAY-181187 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [540213], [548017] | |
Inhibitor | (+/-)-nantenine | Drug Info | [530558] | ||
1-(2-Methoxy-phenyl)-piperazine | Drug Info | [527463] | |||
1-(3-(benzyloxy)-2-methylphenyl)piperazine | Drug Info | [530058] | |||
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [529013] | |||
1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole | Drug Info | [527760] | |||
1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole | Drug Info | [527703] | |||
1-Benzenesulfonyl-3-piperidin-4-yl-1H-indole | Drug Info | [527339] | |||
1-Naphthalen-1-yl-piperazine | Drug Info | [527463] | |||
1-phenylthio-N,N-dimethyltryptamine | Drug Info | [529258] | |||
2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine | Drug Info | [529112] | |||
2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine | Drug Info | [529929] | |||
2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine | Drug Info | [529929] | |||
2-(1-tosyl-1H-indol-3-yl)ethanamine | Drug Info | [529112] | |||
2-(3-(phenylsulfonyl)-1H-indol-1-yl)ethanamine | Drug Info | [530209] | |||
2-(3-benzenesulfonyl)phenyl-1-aminoethane | Drug Info | [528373] | |||
2-(3-phenylthio)phenyl)-1-aminoethane | Drug Info | [528373] | |||
2-(4-(benzenesulfonyl)phenyl)-1-aminoethane | Drug Info | [528373] | |||
2-Benzyl-4-piperazin-1-yl-1H-benzimidazole | Drug Info | [530637] | |||
2-Ethyl-5-methoxy-3-piperidin-4-yl-1H-indole | Drug Info | [527665] | |||
3-(2-Amino-ethyl)-2-methyl-1H-indol-5-ol | Drug Info | [526655] | |||
3-(phenylsulfonyl)-1-(piperidin-3-yl)-1H-indole | Drug Info | [530698] | |||
3-(phenylsulfonyl)-1-(piperidin-4-yl)-1H-indole | Drug Info | [530698] | |||
3-(phenylsulfonyl)-1-(pyrrolidin-3-yl)-1H-indole | Drug Info | [530698] | |||
4-((1H-indol-1-yl)methyl)benzenamine | Drug Info | [528630] | |||
4-(1H-Inden-1-ylmethyl)-phenylamine | Drug Info | [527501] | |||
4-(1H-indol-1-ylsulfonyl)benzenamine | Drug Info | [527760] | |||
4-(1H-Indol-3-ylmethyl)-phenylamine | Drug Info | [527501] | |||
4-(2-benzenesulfonylphenyl)piperazine | Drug Info | [528373] | |||
4-(3-benzenesulfonamidophenyl)piperazine | Drug Info | [528373] | |||
4-(3-benzenesulfonylphenyl)piperazine | Drug Info | [528373] | |||
4-(3-Methyl-indole-1-sulfonyl)-phenylamine | Drug Info | [527463] | |||
4-(3H-Inden-1-ylmethyl)-phenylamine | Drug Info | [527501] | |||
4-(4,6-dinitro-1H-indol-1-ylsulfonyl)benzenamine | Drug Info | [527760] | |||
4-(4-benzenesulfonamidophenyl)piperazine | Drug Info | [528373] | |||
4-(4-benzenesulfonylphenyl)piperazine | Drug Info | [528373] | |||
4-(4-methoxy-1H-indol-1-ylsulfonyl)benzenamine | Drug Info | [528206] | |||
4-(6-methoxy-1H-indol-1-ylsulfonyl)benzenamine | Drug Info | [528206] | |||
4-(Indan-1-ylsulfanyl)-phenylamine | Drug Info | [527501] | |||
4-(Indane-1-sulfonyl)-phenylamine | Drug Info | [527501] | |||
4-(Naphthalene-1-sulfonyl)-phenylamine | Drug Info | [527463] | |||
4-(piperazin-1-yl)-1H-indole | Drug Info | [527760] | |||
4-(piperazin-1-yl)-3-tosyl-1H-indazole | Drug Info | [531198] | |||
4-Indan-1-ylmethyl-phenylamine | Drug Info | [527501] | |||
4-Inden-(1E)-ylidenemethyl-phenylamine | Drug Info | [527501] | |||
5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
5-(4-Methylpiperazin-1-yl)-3-tosyl-1H-indazole | Drug Info | [531198] | |||
5-MEO-DMT | Drug Info | [528416] | |||
5-METHOXYTRYPTAMINE | Drug Info | [527474] | |||
6-(piperazin-1-yl)-3-tosyl-1H-indazole | Drug Info | [531198] | |||
6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole | Drug Info | [529564] | |||
CHLOROPHENYLPIPERAZINE | Drug Info | [526655] | |||
DIMEBOLIN | Drug Info | [530540] | |||
Dimethyltryptamine | Drug Info | [551401] | |||
E-6837 | Drug Info | [529929] | |||
EDMT | Drug Info | [529929] | |||
METHIOTHEPIN | Drug Info | [530739] | |||
N,N-diethyl-2-(1H-indol-3-yl)ethanamine | Drug Info | [528416] | |||
N,N-dimethyl-2-(1-tosyl-1H-indol-3-yl)ethanamine | Drug Info | [528630] | |||
N-(3-(2-aminoethyl)phenyl)benzenesulfonamide | Drug Info | [528373] | |||
N-(3-(3-aminopropyl)phenyl)benzenesulfonamide | Drug Info | [528373] | |||
N-(3-(aminomethyl)phenyl)benzenesulfonamide | Drug Info | [528373] | |||
N-(3-aminophenyl)benzenesulfonamide | Drug Info | [528373] | |||
N-(4-(2-aminoethyl)phenyl)benzenesulfonamide | Drug Info | [528373] | |||
N-phenyl-3-(2-aminoethyl)benzenesulfonamide | Drug Info | [528373] | |||
OCTOCLOTHEPIN | Drug Info | [527474] | |||
QUIPAZINE | Drug Info | [526655] | |||
Ro-04-6790 | Drug Info | [529929] | |||
Ro-63-0563 | Drug Info | [529191] | |||
SB-271046 | Drug Info | [530058] | |||
SB-357134 | Drug Info | [529191] | |||
SEROTONIN | Drug Info | [530739] | |||
SPIPERONE | Drug Info | [526655] | |||
WAY-208466 | Drug Info | [530209] | |||
WAY-466 | Drug Info | [527381] | |||
[2-(3-Benzyl-3H-inden-1-yl)-ethyl]-methyl-amine | Drug Info | [527501] | |||
[2-(3-Benzyl-3H-indol-1-yl)-ethyl]-dimethyl-amine | Drug Info | [527212] | |||
[2-(3-Benzyl-indol-1-yl)-ethyl]-dimethyl-amine | Drug Info | [527501] | |||
[2-(3H-Indol-1-yl)-ethyl]-dimethyl-amine | Drug Info | [527212] | |||
Agonist | 1-naphthylpiperazine | Drug Info | [533689] | ||
2-methyl-5-HT | Drug Info | [534430] | |||
5-CT | Drug Info | [534065] | |||
alpha-methyl-5-HT | Drug Info | [534734] | |||
BRL-15572 | Drug Info | [534475] | |||
DM-1451 | Drug Info | [525492] | |||
E6801 | Drug Info | [527474] | |||
EMD-386088 | Drug Info | [527665] | |||
EMDT | Drug Info | [525722] | |||
lergotrile | Drug Info | [533689] | |||
LY 165,163 | Drug Info | [533689] | |||
m-chlorophenylpiperazine | Drug Info | [533689] | |||
OPC 4392 | Drug Info | [525492] | |||
TFMPP | Drug Info | [533689] | |||
[3H]5-CT | Drug Info | [543365] | |||
[3H]LSD | Drug Info | [525492] | |||
Antagonist | 11C-GSK-215083 | Drug Info | [531758] | ||
2-bromo-LSD | Drug Info | [533689] | |||
5-HT 6 antagonists | Drug Info | [543365] | |||
5-HT 6 receptor antagonists | Drug Info | [543365] | |||
alpha-ergocryptine | Drug Info | [534734] | |||
AVN 397 | Drug Info | [544229] | |||
bufotenine | Drug Info | [534430] | |||
BVT-74316 | Drug Info | [544074] | |||
fluperlapine | Drug Info | [533798] | |||
metergoline | Drug Info | [534703] | |||
MPDT | Drug Info | [525722] | |||
PF-05212377 | Drug Info | [550237] | |||
PRX-07034 | Drug Info | [533042] | |||
SAM-531 | Drug Info | [532199] | |||
SB 258585 | Drug Info | [535506] | |||
SB-742457 | Drug Info | [544323], [550963] | |||
SB399885 | Drug Info | [528500] | |||
SUVN-501 | Drug Info | [543365] | |||
SUVN-502 | Drug Info | [544399] | |||
SUVN-504 | Drug Info | [543365] | |||
SUVN-507 | Drug Info | [543365] | |||
SYN-114 | Drug Info | [544005] | |||
SYN-120 | Drug Info | [544216] | |||
[125I]SB-258585 | Drug Info | [535506] | |||
[3H]Ro 63-0563 | Drug Info | [534703] | |||
Modulator | ABT-354 | Drug Info | [549319] | ||
AMR-SIX-1 | Drug Info | [543365] | |||
AVN 101 | Drug Info | [544229] | |||
AVN 211 | Drug Info | [544229] | |||
AVN 322 | Drug Info | [544323] | |||
SB-214111 | Drug Info | ||||
SEL-73 | Drug Info | [543365] | |||
WAY-181187 | Drug Info | ||||
Enhancer | LU AE58054 | Drug Info | [530983] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
cAMP signaling pathway | |||||
Neuroactive ligand-receptor interaction | |||||
Serotonergic synapse | |||||
PANTHER Pathway | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | ||||
PathWhiz Pathway | Excitatory Neural Signalling Through 5-HTR 6 and Serotonin | ||||
Reactome | Serotonin receptors | ||||
G alpha (s) signalling events | |||||
WikiPathways | Serotonin Receptor 4/6/7 and NR3C Signaling | ||||
Monoamine GPCRs | |||||
GPCRs, Class A Rhodopsin-like | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 522658 | 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 524103 | 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 524382 | 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 524945 | 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 525385 | List of drugs in development for neurodegenerative diseases: update October 2011. Neurodegener Dis. 2012;9(4):210-83. | ||||
Ref 540213 | (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 542377 | (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 543132 | (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 543246 | (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 547850 | 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 547877 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020107) | ||||
Ref 548017 | 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 548037 | 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 548202 | 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 548444 | 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 548881 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029827) | ||||
Ref 548893 | 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 549022 | 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 525492 | Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology. 1999 Jun;20(6):612-27. | ||||
Ref 525722 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8. | ||||
Ref 526655 | J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). | ||||
Ref 527212 | Bioorg Med Chem Lett. 2004 Sep 6;14(17):4569-73.Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors. | ||||
Ref 527339 | Bioorg Med Chem Lett. 2005 Jan 17;15(2):379-83.N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. | ||||
Ref 527381 | J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. | ||||
Ref 527463 | Bioorg Med Chem Lett. 2005 Mar 15;15(6):1707-11.1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. | ||||
Ref 527474 | J Med Chem. 2005 Mar 24;48(6):1781-95.Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. | ||||
Ref 527501 | Bioorg Med Chem Lett. 2005 Apr 15;15(8):1987-91.Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. | ||||
Ref 527665 | Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4.2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. | ||||
Ref 527703 | Bioorg Med Chem Lett. 2005 Nov 1;15(21):4780-5.Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists. | ||||
Ref 527760 | Bioorg Med Chem Lett. 2005 Dec 1;15(23):5298-302. Epub 2005 Sep 23.Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. | ||||
Ref 528206 | Bioorg Med Chem Lett. 2006 Jul 15;16(14):3793-6. Epub 2006 May 18.Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. | ||||
Ref 528373 | J Med Chem. 2006 Aug 24;49(17):5217-25.Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. | ||||
Ref 528416 | Bioorg Med Chem Lett. 2006 Nov 15;16(22):5832-5. Epub 2006 Aug 30.Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. | ||||
Ref 528500 | SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. Eur J Pharmacol. 2006 Dec 28;553(1-3):109-19. Epub 2006 Sep 29. | ||||
Ref 528630 | Bioorg Med Chem Lett. 2007 Mar 15;17(6):1691-4. Epub 2007 Jan 4.Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors. | ||||
Ref 529013 | Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. | ||||
Ref 529112 | J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.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. | ||||
Ref 529148 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. | ||||
Ref 529191 | Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. | ||||
Ref 529258 | J Med Chem. 2008 Feb 14;51(3):603-11. Epub 2008 Jan 18.Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. | ||||
Ref 529564 | Bioorg Med Chem Lett. 2008 Jul 15;18(14):3929-31. Epub 2008 Jun 13.A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands. | ||||
Ref 529929 | J Med Chem. 2009 Feb 12;52(3):675-87.Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. | ||||
Ref 530058 | Bioorg Med Chem Lett. 2009 May 1;19(9):2409-12. Epub 2009 Mar 25.Synthesis and SAR of tolylamine 5-HT6 antagonists. | ||||
Ref 530209 | Bioorg Med Chem. 2009 Jul 15;17(14):5153-63. Epub 2009 May 29.Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. | ||||
Ref 530540 | Eur J Med Chem. 2010 Feb;45(2):782-9. Epub 2009 Oct 31.8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. | ||||
Ref 530558 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. | ||||
Ref 530637 | J Med Chem. 2010 Feb 11;53(3):1357-69.Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation. | ||||
Ref 530698 | Bioorg Med Chem Lett. 2010 Mar 1;20(5):1657-60. Epub 2010 Jan 21.3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators. | ||||
Ref 530739 | J Med Chem. 2010 Mar 25;53(6):2521-7.5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. | ||||
Ref 530983 | 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 531198 | J Med Chem. 2010 Nov 11;53(21):7639-46.5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. | ||||
Ref 531758 | 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 532199 | Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9. | ||||
Ref 533042 | 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 533689 | Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol. 1993 Mar;43(3):320-7. | ||||
Ref 533798 | 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 534065 | Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem. 1996 Jan;66(1):47-56. | ||||
Ref 534430 | Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells. Neuropharmacology. 1997 Apr-May;36(4-5):713-20. | ||||
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