General Information of Drug Therapeutic Target (DTT) (ID: TTO9X1H)

DTT Name 5-HT 7 receptor (HTR7)
Synonyms Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
Gene Name HTR7
DTT Type
Clinical trial target
[1]
BioChemical Class
GPCR rhodopsin
UniProt ID
5HT7R_HUMAN
TTD ID
T79062
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MMDVNSSGRPDLYGHLRSFLLPEVGRGLPDLSPDGGADPVAGSWAPHLLSEVTASPAPTW
DAPPDNASGCGEQINYGRVEKVVIGSILTLITLLTIAGNCLVVISVCFVKKLRQPSNYLI
VSLALADLSVAVAVMPFVSVTDLIGGKWIFGHFFCNVFIAMDVMCCTASIMTLCVISIDR
YLGITRPLTYPVRQNGKCMAKMILSVWLLSASITLPPLFGWAQNVNDDKVCLISQDFGYT
IYSTAVAFYIPMSVMLFMYYQIYKAARKSAAKHKFPGFPRVEPDSVIALNGIVKLQKEVE
ECANLSRLLKHERKNISIFKREQKAATTLGIIVGAFTVCWLPFFLLSTARPFICGTSCSC
IPLWVERTFLWLGYANSLINPFIYAFFNRDLRTTYRSLLQCQYRNINRKLSAAGMHEALK
LAERPERPEFVLRACTRRVLLRPEKRPPVSVWVLQSPDHHNWLADKMLTTVEKKVMIHD
Function
The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. 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.
KEGG Pathway
Ras signaling pathway (hsa04014 )
Calcium signaling pathway (hsa04020 )
Neuroactive ligand-receptor interaction (hsa04080 )
Serotonergic synapse (hsa04726 )
Reactome Pathway
G alpha (s) signalling events (R-HSA-418555 )
Serotonin receptors (R-HSA-390666 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
4 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AVN-101 DMOGFNI Cognitive impairment 6D71 Phase 2 [2]
JNJ-18038683 DMV1T59 Major depressive disorder 6A70.3 Phase 2 [3]
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [4]
ATI-9242 DM6GKMU Schizophrenia 6A20 Phase 1 [5]
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4 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
4-oxadiazole derivative 1 DMWFHKR N. A. N. A. Patented [6]
Carbamide derivative 2 DMW5GI3 N. A. N. A. Patented [6]
PMID30124346-Compound-13TABLE4 DMHTJVA Attention deficit hyperactivity disorder 6A05.Z Patented [7]
PMID30124346-Compound-34TABLE4 DM2G3VE Attention deficit hyperactivity disorder 6A05.Z Patented [7]
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1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
SB-269970 DM8WTGA Sleep-wake disorder 7A00-7B2Z Terminated [8]
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63 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(+/-)-nantenine DM0L3GE Discovery agent N.A. Investigative [9]
(2-biphenyl-3-yl-ethyl)-dimethyl-amine DMTW0GD Discovery agent N.A. Investigative [10]
(R)-8-phenyl-N,N-dipropylchroman-3-amine DMCY76E Discovery agent N.A. Investigative [11]
1-(2-Methoxy-phenyl)-piperazine DM3M4RA Discovery agent N.A. Investigative [12]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine DMX5N3V Discovery agent N.A. Investigative [13]
1-naphthylpiperazine DM6BIWK Discovery agent N.A. Investigative [1]
2-(1-o-tolyl-1H-pyrrol-3-yl)ethanamine DMY35HG Discovery agent N.A. Investigative [10]
2-(2'-methyl-biphenyl-3-yl)-ethylamine DM7HN4Z Discovery agent N.A. Investigative [10]
2-(2-Bromophenoxy)-N,N-dimethylethanamine DMHBE0X Discovery agent N.A. Investigative [11]
2-(2-Bromophenylthio)-N,N-dimethylethanamine DMHJMUX Discovery agent N.A. Investigative [11]
2-(Biphenyl-2-yloxy)-N,N-dimethylethanamine DM0C5O3 Discovery agent N.A. Investigative [11]
2-(Biphenyl-2-ylthio)-N,N-dimethylethanamine DM9XZSC Discovery agent N.A. Investigative [11]
2-bromo-LSD DMOYCWU Discovery agent N.A. Investigative [14]
2-[1-(2-Chloro-phenyl)-1H-pyrrol-2-yl]-ethylamine DMSW89U Discovery agent N.A. Investigative [15]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [16]
5,6-dichloro-3,4-dihydroquinazolin-2-amine DMN1S35 Discovery agent N.A. Investigative [17]
5-chloro-3,4-dihydroquinazolin-2-amine DMKEFJ0 Discovery agent N.A. Investigative [17]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine DMGDTNI Discovery agent N.A. Investigative [17]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine DM7FZU2 Discovery agent N.A. Investigative [17]
5-CT DM260KD Discovery agent N.A. Investigative [14]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine DMK6U2V Discovery agent N.A. Investigative [17]
AS-19 DMASE5O Discovery agent N.A. Investigative [18]
bufotenine DMD1SY9 Discovery agent N.A. Investigative [14]
cyamemazine DMZ6YPV Discovery agent N.A. Investigative [19]
dihydroergocryptine DMDW2NL Discovery agent N.A. Investigative [14]
dipropyl-5-CT DM9VKXC Discovery agent N.A. Investigative [20]
Disulergine DM6TVAX Discovery agent N.A. Investigative [21]
DM-1451 DMM0VDK Discovery agent N.A. Investigative [22]
DR-4004 DMW8ORN Discovery agent N.A. Investigative [21]
E55888 DM0O8KR Discovery agent N.A. Investigative [23]
EDMT DMS3AXK Discovery agent N.A. Investigative [24]
Elaidoylamide DMP8VDT Discovery agent N.A. Investigative [25]
FALCARINDIOL DMLOV18 Discovery agent N.A. Investigative [26]
fluperlapine DM9KIPU Discovery agent N.A. Investigative [27]
IMPERATORIN DMVLW6R Discovery agent N.A. Investigative [26]
LP-12 DM8ZR17 Discovery agent N.A. Investigative [28]
LP-211 DMKDGLA Discovery agent N.A. Investigative [29]
LP-44 DM0C3SF Discovery agent N.A. Investigative [28]
m-chlorophenylpiperazine DMM1J2D Discovery agent N.A. Investigative [12]
MESULERGINE DMKGWAH Discovery agent N.A. Investigative [30]
METHIOTHEPIN DMMC0I7 Discovery agent N.A. Investigative [31]
MPDT DMYX31S Discovery agent N.A. Investigative [24]
N,N-dimethyl-2-(2'-methylbiphenyl-3-yl)ethanamine DM1DZEL Discovery agent N.A. Investigative [11]
N-methyl-Pip-F-homoF-vinyl sulfonyl phenyl (N-methyl-Pip-F-hF-VS phi) DMDAN0K Discovery agent N.A. Investigative [32]
OPC 4392 DMQOJY2 Discovery agent N.A. Investigative [22]
P-hydroxyphenethyl trans-ferulate DMPS1Y2 Discovery agent N.A. Investigative [26]
pirenperone DM9T2G3 Discovery agent N.A. Investigative [20]
SB 269970-A DMFHUGC Discovery agent N.A. Investigative [32]
SB-258719 DMO01AG Discovery agent N.A. Investigative [21]
SB-258741 DM0HK6L Discovery agent N.A. Investigative [21]
SB-271046 DM5VJAF Discovery agent N.A. Investigative [33]
SB-656104 DMVOIL5 Discovery agent N.A. Investigative [21]
SEL-73 DMFKE6C Psychiatric disorder 6E8Z Investigative [34]
SEROTONIN DMOFCRY Discovery agent N.A. Investigative [35]
TFMPP DMAC8TP Discovery agent N.A. Investigative [12]
UCM-5600 DMOJ4TG Discovery agent N.A. Investigative [30]
WAY-208466 DM9K2LU Discovery agent N.A. Investigative [36]
WAY-466 DMMOH51 Discovery agent N.A. Investigative [37]
[125I]LSD DMP69QG Discovery agent N.A. Investigative [38]
[3H]5-CT DMEAHFZ Discovery agent N.A. Investigative [8]
[3H]5-HT DMYJXV7 Discovery agent N.A. Investigative [1]
[3H]LSD DM0YJHS Discovery agent N.A. Investigative [39]
[3H]spiperone DMWHEV8 Discovery agent N.A. Investigative [21]
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⏷ Show the Full List of 63 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Major depressive disorder 6A20 Pre-frontal cortex 9.79E-01 -0.08 -0.32
Schizophrenia 6A20 Pre-frontal cortex 4.97E-02 -0.03 -0.11
Schizophrenia 6A20 Superior temporal cortex 3.78E-01 -4.84E-04 -3.66E-03
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References

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4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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6 Acyltransferase inhibitors: a patent review (2010-present).Expert Opin Ther Pat. 2015 Feb;25(2):145-58.
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12 Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. J Biol Chem. 1993 Aug 25;268(24):18200-4.
13 The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66.
14 Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. Mol Pharmacol. 1993 Aug;44(2):229-36.
15 Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2005 Aug 15;15(16):3753-7.
16 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.
17 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.
18 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.
19 Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
20 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.
21 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
22 Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology. 1999 Jun;20(6):612-27.
23 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain. 2009 Feb;141(3):239-47.
24 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
25 Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine7 receptors. Biochem Pharmacol. 1999 Dec 1;58(11):1807-13.
26 Serotonergic activity-guided phytochemical investigation of the roots of Angelica sinensis. J Nat Prod. 2006 Apr;69(4):536-41.
27 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.
28 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.
29 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.
30 Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. J Med Chem. 2009 Apr 23;52(8):2384-92.
31 Novel quinazolinone derivatives as 5-HT7 receptor ligands. Bioorg Med Chem. 2008 Mar 1;16(5):2570-8.
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33 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.
34 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: 12).
35 Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
36 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.
37 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.
38 A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. Neuron. 1993 Sep;11(3):449-58.
39 Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants. FEBS Lett. 1997 Aug 25;413(3):489-94.