5-hydroxytryptamine receptor 5A
Also known as: HTR5A
Function
G protein-coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen. Also functions as a receptor for ergot alkaloid derivatives and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. HTR5A is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission: signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores.
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- 5HT5A_rcpt, 5HT_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
- Functional cluster
- G Protein-Coupled Receptors
Experimental structures · PDB · 6
A predicted model is available from AlphaFold.
Gene Ontology · 14
- GO:0030425 dendrite
- GO:0043204 perikaryon
- GO:0005886 plasma membrane
- GO:0099634 postsynaptic specialization membrane
- GO:0004993 G protein-coupled serotonin receptor activity
- GO:0001586 Gi/o-coupled serotonin receptor activity
- GO:0030594 neurotransmitter receptor activity
- GO:0099589 serotonin receptor activity
- GO:0007198 adenylate cyclase-inhibiting serotonin receptor signaling pathway
- GO:0007268 chemical synaptic transmission
- GO:0007186 G protein-coupled receptor signaling pathway
- GO:0007187 G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
- GO:0021766 hippocampus development
- GO:0032355 response to estradiol
Drugs targeting this protein · 3
- DEXFENFLURAMINE HYDROCHLORIDE agonist
- ZIMELDINE HYDROCHLORIDE antagonist
- AMISULPRIDE antagonist
Related proteins · sequence + function similarity
- 5-hydroxytryptamine receptor 5A 0.99
- 5-hydroxytryptamine receptor 5A 0.99
- 5-hydroxytryptamine receptor 5B 0.95
- 5-hydroxytryptamine receptor 5B 0.95
- D(1)-like dopamine receptor 0.93
- D(3) dopamine receptor 0.93
- D(3) dopamine receptor 0.93
- 5-hydroxytryptamine receptor 1D 0.93
- D(3) dopamine receptor 0.93
- 5-hydroxytryptamine receptor 1D 0.93
- 5-hydroxytryptamine receptor 1D 0.92
- 5-hydroxytryptamine receptor 1B 0.92
Co-cited proteins · studied together in the literature
- Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 2 shared papers
- Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 2 shared papers
- 5-hydroxytryptamine receptor 1F 1 shared papers
- 5-hydroxytryptamine receptor 1E 1 shared papers
- 5-hydroxytryptamine receptor 1B 1 shared papers
- 5-hydroxytryptamine receptor 1A 1 shared papers
- Guanine nucleotide-binding protein G(i) subunit alpha-1 1 shared papers
Literature · 6 cited papers
- Inactive and active state structures template selective tools for the human 5-HT5A receptor. Nat. Struct. Mol. Biol. · 2022
- Structural insights into the ligand binding and Gi coupling of serotonin receptor 5-HT5A. Cell Discov. · 2022
- The consensus coding sequences of human breast and colorectal cancers. Science · 2006
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells. Eur. J. Pharmacol. · 1998
- Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. · 1994