lmmol · Proteins

5-hydroxytryptamine receptor 2A

UniProt P28223 Organism Homo sapiens Gene HTR2, HTR2A

Also known as: HTR2, HTR2A

Function

G protein-coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. HTR2A is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction (By similarity).

Classification

Family (Pfam)
PF00001 7tm_1
InterPro
5HT2A_rcpt, 5HT_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster
Membrane Transporters & GPCRs

Experimental structures · PDB · 37

A predicted model is available from AlphaFold.

Gene Ontology · 55

Drugs targeting this protein · 63

Neighborhood · nearest proteins

HTR2HTR2AHTR2AHTR2AHTR1CHTR2BGPRC1B
Nearest neighbours of 5-hydroxytryptamine receptor 2A: 3 by sequence/function similarity (left); 3 co-cited in the literature (right).

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Literature · 25 cited papers

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