Target Information
Target General Infomation | |||||
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Target ID |
T79062
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Former ID |
TTDR00157
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Target Name |
5-hydroxytryptamine 7 receptor
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Gene Name |
HTR7
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Synonyms |
5-HT-7; 5-HT-X; 5-HT7 receptor; 5HT7; Serotonin receptor; Serotonin receptor 7; HTR7
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Target Type |
Clinical Trial
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Disease | Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | ||||
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10: F51, G47] | |||||
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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T79062
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UniProt ID | |||||
Sequence |
MMDVNSSGRPDLYGHLRSFLLPEVGRGLPDLSPDGGADPVAGSWAPHLLSEVTASPAPTW
DAPPDNASGCGEQINYGRVEKVVIGSILTLITLLTIAGNCLVVISVCFVKKLRQPSNYLI VSLALADLSVAVAVMPFVSVTDLIGGKWIFGHFFCNVFIAMDVMCCTASIMTLCVISIDR YLGITRPLTYPVRQNGKCMAKMILSVWLLSASITLPPLFGWAQNVNDDKVCLISQDFGYT IYSTAVAFYIPMSVMLFMYYQIYKAARKSAAKHKFPGFPRVEPDSVIALNGIVKLQKEVE ECANLSRLLKHERKNISIFKREQKAATTLGIIVGAFTVCWLPFFLLSTARPFICGTSCSC IPLWVERTFLWLGYANSLINPFIYAFFNRDLRTTYRSLLQCQYRNINRKLSAAGMHEALK LAERPERPEFVLRACTRRVLLRPEKRPPVSVWVLQSPDHHNWLADKMLTTVEKKVMIHD |
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Drugs and Mode of Action | |||||
Drug(s) | JNJ-18038683 | Drug Info | Phase 2 | Major depressive disorder | [1], [2] |
ATI-9242 | Drug Info | Discontinued in Phase 2 | Schizophrenia | [3] | |
SB-269970 | Drug Info | Terminated | Sleep disorders | [4], [5] | |
Agonist | (+)-LSD | Drug Info | [6] | ||
1-naphthylpiperazine | Drug Info | [7] | |||
2-MPP | Drug Info | [8] | |||
5-CT | Drug Info | [9] | |||
AS-19 | Drug Info | [10] | |||
bufotenine | Drug Info | [9] | |||
dipropyl-5-CT | Drug Info | [11] | |||
DM-1451 | Drug Info | [12] | |||
E55888 | Drug Info | [13] | |||
EMDT | Drug Info | [14] | |||
LP-12 | Drug Info | [15] | |||
LP-211 | Drug Info | [16] | |||
LP-44 | Drug Info | [15] | |||
m-chlorophenylpiperazine | Drug Info | [8] | |||
OPC 4392 | Drug Info | [12] | |||
TFMPP | Drug Info | [8] | |||
[125I]LSD | Drug Info | [17] | |||
[3H]5-CT | Drug Info | [18] | |||
[3H]5-HT | Drug Info | [7] | |||
[3H]LSD | Drug Info | [19] | |||
Inhibitor | (+/-)-nantenine | Drug Info | [20] | ||
(2-biphenyl-3-yl-ethyl)-dimethyl-amine | Drug Info | [21] | |||
(R)-8-phenyl-N,N-dipropylchroman-3-amine | Drug Info | [22] | |||
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [23] | |||
1-Naphthalen-1-yl-piperazine | Drug Info | [24] | |||
2-(1-o-tolyl-1H-pyrrol-3-yl)ethanamine | Drug Info | [21] | |||
2-(2'-methyl-biphenyl-3-yl)-ethylamine | Drug Info | [21] | |||
2-(2-Bromophenoxy)-N,N-dimethylethanamine | Drug Info | [22] | |||
2-(2-Bromophenylthio)-N,N-dimethylethanamine | Drug Info | [22] | |||
2-(Biphenyl-2-yloxy)-N,N-dimethylethanamine | Drug Info | [22] | |||
2-(Biphenyl-2-ylthio)-N,N-dimethylethanamine | Drug Info | [22] | |||
2-[1-(2-Chloro-phenyl)-1H-pyrrol-2-yl]-ethylamine | Drug Info | [25] | |||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [26] | |||
5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [27] | |||
5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [27] | |||
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [27] | |||
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [27] | |||
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [27] | |||
Disulergine | Drug Info | [24] | |||
FALCARINDIOL | Drug Info | [28] | |||
IMPERATORIN | Drug Info | [28] | |||
MESULERGINE | Drug Info | [29] | |||
METHIOTHEPIN | Drug Info | [30] | |||
N,N-dimethyl-2-(2'-methylbiphenyl-3-yl)ethanamine | Drug Info | [22] | |||
P-hydroxyphenethyl trans-ferulate | Drug Info | [28] | |||
SB-258719 | Drug Info | [24] | |||
SB-258741 | Drug Info | [24] | |||
SB-271046 | Drug Info | [31] | |||
SB-656104 | Drug Info | [24] | |||
SEROTONIN | Drug Info | [32] | |||
SPIPERONE | Drug Info | [24] | |||
UCM-5600 | Drug Info | [29] | |||
WAY-208466 | Drug Info | [33] | |||
WAY-466 | Drug Info | [34] | |||
Antagonist | 2-bromo-LSD | Drug Info | [9] | ||
cyamemazine | Drug Info | [35] | |||
dihydroergocryptine | Drug Info | [9] | |||
DR-4004 | Drug Info | [24] | |||
fluperlapine | Drug Info | [36] | |||
JNJ-18038683 | Drug Info | [37] | |||
metergoline | Drug Info | [7] | |||
MPDT | Drug Info | [14] | |||
pirenperone | Drug Info | [11] | |||
SB 269970-A | Drug Info | [38] | |||
SB 656104-A | Drug Info | [38] | |||
[3H]SB269970 | Drug Info | [18] | |||
Modulator | ATI-9242 | Drug Info | [39] | ||
SB-269970 | Drug Info | ||||
SEL-73 | Drug Info | [40] | |||
Modulator (allosteric modulator) | oleamide | Drug Info | [41] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Ras signaling pathway | ||||
Calcium 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 7 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 | |||||
GPCRs, Other | |||||
References | |||||
REF 1 | ClinicalTrials.gov (NCT00566202) A Safety and Effectiveness Study of JNJ-18038683 in Patients With Moderate to Severe Depression. U.S. National Institutes of Health. | ||||
REF 2 | (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: 8432). | ||||
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 800028165) | ||||
REF 4 | (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: 3233). | ||||
REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017732) | ||||
REF 6 | Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. Proc Natl Acad Sci U S A. 1993 Sep 15;90(18):8547-51. | ||||
REF 7 | Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. | ||||
REF 8 | Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. J Biol Chem. 1993 Aug 25;268(24):18200-4. | ||||
REF 9 | Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. Mol Pharmacol. 1993 Aug;44(2):229-36. | ||||
REF 10 | Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor. Bioorg Med Chem. 2013 May 1;21(9):2568-76. | ||||
REF 11 | Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b). Br J Pharmacol. 1997 Sep;122(1):126-32. | ||||
REF 12 | Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology. 1999 Jun;20(6):612-27. | ||||
REF 13 | 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain. 2009 Feb;141(3):239-47. | ||||
REF 14 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8. | ||||
REF 15 | Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21. Epub 2007 Jul 25. | ||||
REF 16 | J Med Chem. 2008 Sep 25;51(18):5813-22.Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. | ||||
REF 17 | A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. Neuron. 1993 Sep;11(3):449-58. | ||||
REF 18 | [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors. Br J Pharmacol. 2000 May;130(2):409-17. | ||||
REF 19 | Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants. FEBS Lett. 1997 Aug 25;413(3):489-94. | ||||
REF 20 | 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 21 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22. Epub 2007 Mar 23.Novel aminoethylbiphenyls as 5-HT7 receptor ligands. | ||||
REF 22 | Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. Epub 2010 Jan 18.SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. | ||||
REF 23 | 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 24 | 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 25 | Bioorg Med Chem Lett. 2005 Aug 15;15(16):3753-7.Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands. | ||||
REF 26 | J Med Chem. 2010 Sep 9;53(17):6386-97.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 receptor agonist with unprecedented selectivity and procognitive potential. | ||||
REF 27 | 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 28 | J Nat Prod. 2006 Apr;69(4):536-41.Serotonergic activity-guided phytochemical investigation of the roots of Angelica sinensis. | ||||
REF 29 | J Med Chem. 2009 Apr 23;52(8):2384-92.Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. | ||||
REF 30 | Bioorg Med Chem. 2008 Mar 1;16(5):2570-8. Epub 2007 Nov 22.Novel quinazolinone derivatives as 5-HT7 receptor ligands. | ||||
REF 31 | 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 32 | J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. | ||||
REF 33 | 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 34 | 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 35 | Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40. | ||||
REF 36 | 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 37 | Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci. 2015 Jan 15;8:453. | ||||
REF 38 | 5-HT7 receptors. Curr Drug Targets CNS Neurol Disord. 2004 Feb;3(1):81-90. | ||||
REF 39 | Pharmacological characteristics of ATI-9242, a Novel Atypical Antipsychotic. FASEB J, April, 2010, 24(Meeting Abstract Supplement),773.12. | ||||
REF 40 | (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: 12). | ||||
REF 41 | Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine7 receptors. Biochem Pharmacol. 1999 Dec 1;58(11):1807-13. |
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