Target Information

Target General Infomation
Target ID
T16691
Former ID
TTDC00185
Target Name
5-hydroxytryptamine 6 receptor
Gene Name
HTR6
Synonyms
5-HT-6; 5-HT6 receptor; Serotonin receptor; Serotonin receptor 6; HTR6
Target Type
Clinical Trial
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).
BioChemical Class
GPCR rhodopsin
Target Validation
T16691
UniProt ID
P50406
Sequence
MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
FNIDPAEPELRPHPLGIPTN
Drugs and Mode of Action
Drug(s) LU AE58054 Drug Info Phase 3 Schizophrenia [1], [2]
AVN 101 Drug Info Phase 2 Alzheimer disease; Anxiety disorder [3]
AVN 211 Drug Info Phase 2 Schizophrenia [4]
PF-05212377 Drug Info Phase 2 Alzheimer disease [5]
SAM-531 Drug Info Phase 2 Alzheimer disease [6], [7]
SB-742457 Drug Info Phase 2 Alzheimer disease; Dementia [8]
SUVN-502 Drug Info Phase 2 Neurological disease [9]
SYN-120 Drug Info Phase 2 Alzheimer disease [10]
11C-GSK-215083 Drug Info Phase 1 Neurodegenerative disease [11], [12]
ABT-354 Drug Info Phase 1 Alzheimer disease [13]
AVN 322 Drug Info Phase 1 Alzheimer disease [14]
BVT-74316 Drug Info Phase 1 Obesity [15]
PRX-07034 Drug Info Phase 1 Obesity [16]
AVN 397 Drug Info Discontinued in Phase 2 Alzheimer disease; Anxiety disorder [17]
SYN-114 Drug Info Discontinued in Phase 1 Cognitive disorders [18]
WAY-181187 Drug Info Discontinued in Phase 1 Anxiety disorder [19], [20]
Inhibitor (+/-)-nantenine Drug Info [21]
1-(2-Methoxy-phenyl)-piperazine Drug Info [22]
1-(3-(benzyloxy)-2-methylphenyl)piperazine Drug Info [23]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [24]
1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole Drug Info [25]
1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole Drug Info [26]
1-Benzenesulfonyl-3-piperidin-4-yl-1H-indole Drug Info [27]
1-Naphthalen-1-yl-piperazine Drug Info [22]
1-phenylthio-N,N-dimethyltryptamine Drug Info [28]
2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine Drug Info [29]
2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine Drug Info [30]
2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine Drug Info [30]
2-(1-tosyl-1H-indol-3-yl)ethanamine Drug Info [29]
2-(3-(phenylsulfonyl)-1H-indol-1-yl)ethanamine Drug Info [31]
2-(3-benzenesulfonyl)phenyl-1-aminoethane Drug Info [32]
2-(3-phenylthio)phenyl)-1-aminoethane Drug Info [32]
2-(4-(benzenesulfonyl)phenyl)-1-aminoethane Drug Info [32]
2-Benzyl-4-piperazin-1-yl-1H-benzimidazole Drug Info [33]
2-Ethyl-5-methoxy-3-piperidin-4-yl-1H-indole Drug Info [34]
3-(2-Amino-ethyl)-2-methyl-1H-indol-5-ol Drug Info [35]
3-(phenylsulfonyl)-1-(piperidin-3-yl)-1H-indole Drug Info [36]
3-(phenylsulfonyl)-1-(piperidin-4-yl)-1H-indole Drug Info [36]
3-(phenylsulfonyl)-1-(pyrrolidin-3-yl)-1H-indole Drug Info [36]
4-((1H-indol-1-yl)methyl)benzenamine Drug Info [37]
4-(1H-Inden-1-ylmethyl)-phenylamine Drug Info [38]
4-(1H-indol-1-ylsulfonyl)benzenamine Drug Info [25]
4-(1H-Indol-3-ylmethyl)-phenylamine Drug Info [38]
4-(2-benzenesulfonylphenyl)piperazine Drug Info [32]
4-(3-benzenesulfonamidophenyl)piperazine Drug Info [32]
4-(3-benzenesulfonylphenyl)piperazine Drug Info [32]
4-(3-Methyl-indole-1-sulfonyl)-phenylamine Drug Info [22]
4-(3H-Inden-1-ylmethyl)-phenylamine Drug Info [38]
4-(4,6-dinitro-1H-indol-1-ylsulfonyl)benzenamine Drug Info [25]
4-(4-benzenesulfonamidophenyl)piperazine Drug Info [32]
4-(4-benzenesulfonylphenyl)piperazine Drug Info [32]
4-(4-methoxy-1H-indol-1-ylsulfonyl)benzenamine Drug Info [39]
4-(6-methoxy-1H-indol-1-ylsulfonyl)benzenamine Drug Info [39]
4-(Indan-1-ylsulfanyl)-phenylamine Drug Info [38]
4-(Indane-1-sulfonyl)-phenylamine Drug Info [38]
4-(Naphthalene-1-sulfonyl)-phenylamine Drug Info [22]
4-(piperazin-1-yl)-1H-indole Drug Info [25]
4-(piperazin-1-yl)-3-tosyl-1H-indazole Drug Info [40]
4-Indan-1-ylmethyl-phenylamine Drug Info [38]
4-Inden-(1E)-ylidenemethyl-phenylamine Drug Info [38]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [41]
5-(4-Methylpiperazin-1-yl)-3-tosyl-1H-indazole Drug Info [40]
5-MEO-DMT Drug Info [42]
5-METHOXYTRYPTAMINE Drug Info [43]
6-(piperazin-1-yl)-3-tosyl-1H-indazole Drug Info [40]
6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole Drug Info [44]
CHLOROPHENYLPIPERAZINE Drug Info [35]
DIMEBOLIN Drug Info [45]
Dimethyltryptamine Drug Info [46]
E-6837 Drug Info [30]
EDMT Drug Info [30]
METHIOTHEPIN Drug Info [47]
N,N-diethyl-2-(1H-indol-3-yl)ethanamine Drug Info [42]
N,N-dimethyl-2-(1-tosyl-1H-indol-3-yl)ethanamine Drug Info [37]
N-(3-(2-aminoethyl)phenyl)benzenesulfonamide Drug Info [32]
N-(3-(3-aminopropyl)phenyl)benzenesulfonamide Drug Info [32]
N-(3-(aminomethyl)phenyl)benzenesulfonamide Drug Info [32]
N-(3-aminophenyl)benzenesulfonamide Drug Info [32]
N-(4-(2-aminoethyl)phenyl)benzenesulfonamide Drug Info [32]
N-phenyl-3-(2-aminoethyl)benzenesulfonamide Drug Info [32]
OCTOCLOTHEPIN Drug Info [43]
QUIPAZINE Drug Info [35]
Ro-04-6790 Drug Info [30]
Ro-63-0563 Drug Info [48]
SB-271046 Drug Info [23]
SB-357134 Drug Info [48]
SEROTONIN Drug Info [47]
SPIPERONE Drug Info [35]
WAY-208466 Drug Info [31]
WAY-466 Drug Info [49]
[2-(3-Benzyl-3H-inden-1-yl)-ethyl]-methyl-amine Drug Info [38]
[2-(3-Benzyl-3H-indol-1-yl)-ethyl]-dimethyl-amine Drug Info [50]
[2-(3-Benzyl-indol-1-yl)-ethyl]-dimethyl-amine Drug Info [38]
[2-(3H-Indol-1-yl)-ethyl]-dimethyl-amine Drug Info [50]
Agonist 1-naphthylpiperazine Drug Info [51]
2-methyl-5-HT Drug Info [52]
5-CT Drug Info [53]
alpha-methyl-5-HT Drug Info [54]
BRL-15572 Drug Info [55]
DM-1451 Drug Info [56]
E6801 Drug Info [43]
EMD-386088 Drug Info [34]
EMDT Drug Info [57]
lergotrile Drug Info [51]
LY 165,163 Drug Info [51]
m-chlorophenylpiperazine Drug Info [51]
OPC 4392 Drug Info [56]
TFMPP Drug Info [51]
[3H]5-CT Drug Info [58]
[3H]LSD Drug Info [56]
Antagonist 11C-GSK-215083 Drug Info [59]
2-bromo-LSD Drug Info [51]
5-HT 6 antagonists Drug Info [58]
5-HT 6 receptor antagonists Drug Info [58]
alpha-ergocryptine Drug Info [54]
AVN 397 Drug Info [60]
bufotenine Drug Info [52]
BVT-74316 Drug Info [61]
fluperlapine Drug Info [62]
metergoline Drug Info [63]
MPDT Drug Info [57]
PF-05212377 Drug Info [64]
PRX-07034 Drug Info [65]
SAM-531 Drug Info [66]
SB 258585 Drug Info [67]
SB-742457 Drug Info [68], [69]
SB399885 Drug Info [70]
SUVN-501 Drug Info [58]
SUVN-502 Drug Info [71]
SUVN-504 Drug Info [58]
SUVN-507 Drug Info [58]
SYN-114 Drug Info [72]
SYN-120 Drug Info [73]
[125I]SB-258585 Drug Info [67]
[3H]Ro 63-0563 Drug Info [63]
Modulator ABT-354 Drug Info [74]
AMR-SIX-1 Drug Info [58]
AVN 101 Drug Info [60]
AVN 211 Drug Info [60]
AVN 322 Drug Info [68]
SB-214111 Drug Info
SEL-73 Drug Info [58]
WAY-181187 Drug Info
Enhancer LU AE58054 Drug Info [75]
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
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REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019915)
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030006)
REF 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029827)
REF 5ClinicalTrials.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 6ClinicalTrials.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 7(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 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020107)
REF 9Clinical pipeline report, company report or official report of Suven Life Sciences.
REF 10ClinicalTrials.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.
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REF 13ClinicalTrials.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 14Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031585)
REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023034)
REF 16Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021329)
REF 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031584)
REF 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025583)
REF 19(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 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021227)
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REF 30J 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 31Bioorg 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 32J Med Chem. 2006 Aug 24;49(17):5217-25.Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors.
REF 33J Med Chem. 2010 Feb 11;53(3):1357-69.Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.
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REF 35J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
REF 36Bioorg 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 37Bioorg 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 38Bioorg Med Chem Lett. 2005 Apr 15;15(8):1987-91.Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
REF 39Bioorg 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 40J Med Chem. 2010 Nov 11;53(21):7639-46.5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.
REF 41Bioorg 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 42Bioorg 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 43J Med Chem. 2005 Mar 24;48(6):1781-95.Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
REF 44Bioorg 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 45Eur 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 46Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects. Arch Gen Psychiatry. 1994 Feb;51(2):85-97.
REF 47J Med Chem. 2010 Mar 25;53(6):2521-7.5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.
REF 48Bioorg 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 49J 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 50Bioorg 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 51Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol. 1993 Mar;43(3):320-7.
REF 52Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells. Neuropharmacology. 1997 Apr-May;36(4-5):713-20.
REF 53Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem. 1996 Jan;66(1):47-56.
REF 54Identification 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 55SB-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 56Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology. 1999 Jun;20(6):612-27.
REF 572-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
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REF 59Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor. J Nucl Med. 2012 Feb;53(2):295-303.
REF 60Latrepirdine, a potential novel treatment for Alzheimer's disease and Huntington's chorea. Curr Opin Investig Drugs. 2010 January; 11(1): 80-91.
REF 61Pharmacological targeting of the serotonergic system for the treatment of obesity. J Physiol. 2009 January 1; 587(Pt 1): 49-60.
REF 62Binding 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 63The 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 64PF-05212377 Alzheimer's Disease (Phase 2). Pfizer.
REF 65Low-dose prazosin in combination with 5-HT6 antagonist PRX-07034 has antipsychotic effects. Can J Physiol Pharmacol. 2015 Jan;93(1):13-21.
REF 66Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9.
REF 675-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 685-HT6 receptors and Alzheimer's disease. Alzheimers Res Ther. 2013; 5(2): 15.
REF 69Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 70SB-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 71Novel 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 72Lewy bodies. Proc Natl Acad Sci U S A. 2006 February 7; 103(6): 1661-1668.
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REF 74Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035134)
REF 75Lu 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.

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