Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: 5-HT 5A receptor (HTR5A)
• Synonyms: Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
• Gene Name: HTR5A
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT5A_HUMAN
• TTD ID: T15571
• Sequence:
  MDLPVNLTSFSLSTPSPLETNHSLGKDDLRPSSPLLSVFGVLILTLLGFLVAATFAWNLL
  VLATILRVRTFHRVPHNLVASMAVSDVLVAALVMPLSLVHELSGRRWQLGRRLCQLWIAC
  DVLCCTASIWNVTAIALDRYWSITRHMEYTLRTRKCVSNVMIALTWALSAVISLAPLLFG
  WGETYSEGSEECQVSREPSYAVFSTVGAFYLPLCVVLFVYWKIYKAAKFRVGSRKTNSVS
  PISEAVEVKDSAKQPQMVFTVRHATVTFQPEGDTWREQKEQRAALMVGILIGVFVLCWIP
  FFLTELISPLCSCDIPAIWKSIFLWLGYSNSFFNPLIYTAFNKNYNSAFKNFFSRQH
• Function: The activity of this receptor is mediated by G proteins. 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:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Serotonergic synapse (hsa04726)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[1]

26 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[2]
3,4-dihydroquinazolin-2-amine hydrobromide	DMUOXHP	Discovery agent	N.A.	Investigative	[3]
4-ethyl-3,4-dihydroquinazolin-2-amine	DMHDN25	Discovery agent	N.A.	Investigative	[3]
4-methyl-N-propyl-3,4-dihydroquinazolin-2-amine	DMN45EH	Discovery agent	N.A.	Investigative	[4]
4-propyl-3,4-dihydroquinazolin-2-amine	DMRYCL6	Discovery agent	N.A.	Investigative	[3]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[3]
5-chloro-3,4-dihydroquinazolin-2-amine	DMKEFJ0	Discovery agent	N.A.	Investigative	[3]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine	DMGDTNI	Discovery agent	N.A.	Investigative	[3]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine	DM7FZU2	Discovery agent	N.A.	Investigative	[3]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[5]
8-chloro-3,4-dihydroquinazolin-2-amine	DM61VJO	Discovery agent	N.A.	Investigative	[3]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine	DMK6U2V	Discovery agent	N.A.	Investigative	[3]
bufotenine	DMD1SY9	Discovery agent	N.A.	Investigative	[5]
EDMT	DMS3AXK	Discovery agent	N.A.	Investigative	[6]
lysergic acid	DM4MGAQ	Discovery agent	N.A.	Investigative	[5]
METHIOTHEPIN	DMMC0I7	Discovery agent	N.A.	Investigative	[7]
MPDT	DMYX31S	Discovery agent	N.A.	Investigative	[6]
N,4-dimethyl-3,4-dihydroquinazolin-2-amine	DMMTQ3N	Discovery agent	N.A.	Investigative	[4]
N,N-dimethyl-3,4-dihydroquinazolin-2-amine	DMI3CUZ	Discovery agent	N.A.	Investigative	[3]
N-butyl-4-methyl-3,4-dihydroquinazolin-2-amine	DMMI8X4	Discovery agent	N.A.	Investigative	[4]
SB 699551	DM82GH9	Discovery agent	N.A.	Investigative	[8]
SB-699551-A	DMLW8BI	Discovery agent	N.A.	Investigative	[9]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[10]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[11]
[125I]LSD	DMP69QG	Discovery agent	N.A.	Investigative	[12]
[3H]5-CT	DMEAHFZ	Discovery agent	N.A.	Investigative	[12]

References

• [1] Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6.
• [2] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
• [3] 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.
• [4] Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. Bioorg Med Chem Lett. 2008 Jan 1;18(1):262-6.
• [5] Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization. FEBS Lett. 1995 Dec 27;377(3):451-6.
• [6] 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
• [7] Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
• [8] Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4014-8.
• [9] 5-ht5A receptors as a therapeutic target. Pharmacol Ther. 2006 Sep;111(3):707-14.
• [10] 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.
• [11] Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. Mol Pharmacol. 1993 Mar;43(3):313-9.
• [12] Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. Eur J Pharmacol. 2001 Apr 27;418(3):157-67.