5-Hydroxytryptamine 4 receptor (IPR001520)

Short name: 5HT4_rcpt

Overlapping homologous superfamilies


Family relationships


5-hydroxytryptamine (5-HT) or serotonin, is a neurotransmitter that it is primarily found in the gastrointestinal (GI) tract, platelets, and in the central nervous system (CNS). It is implicated in a vast array of physiological and pathophysiological pathways. Receptors for 5-HT mediate both excitatory and inhibitory neurotransmission, and modulate the release of many neurotransmitters including glutamate, GABA, dopamine, epinephrine/norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin and cortisol. In the CNS, 5-HT receptors can influence various neurological processes, such as aggression, anxiety and appetite and, as a, result are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics and anorectics [PMID: 18476671].

The 5-HT receptors are grouped into a number of distinct subtypes, classified according to their antagonist susceptibilities and their affinities for 5-HT. With the exception of the 5-HT3 receptor, which is a ligand-gated ion channel [PMID: 11989819], all 5-HT receptors are members of the rhodopsin-like G protein-coupled receptor family [PMID: 18476671], and they activate an intracellular second messenger cascade to produce their responses.

The 5-HT4 receptor functions in both the peripheral and central nervous system, and is involved in modulating the release of various neurotransmitters. In addition to adenylyl cyclase stimulation, direct coupling to potassium channels and voltage sensitive calcium channels have been proposed as postreceptor events [PMID: 9566034]. The 5HT4 receptor is located in neurons in the CNS, with highest levels in colliculus [PMID: 8219020] and hippocampus [PMID: 7984292, PMID: 10700024, PMID: 7984292, PMID: 8164518], it has not been found in the cerebellum [PMID: 12888181]. In the CNS, the receptor enhances synaptic transmission [PMID: 11986365], and they may also play a role in learning, memory [PMID: 9077568, PMID: 9225295, PMID: 9732367] and appetite [PMID: 15146954]. In the periphery, it is found in the alimentary tract, urinary bladder, heart and adrenal gland [PMID: 8903510, PMID: 9831890, PMID: 10683202, PMID: 9603189].

GO terms

Biological Process

GO:0007186 G protein-coupled receptor signaling pathway
GO:0007268 chemical synaptic transmission
GO:0032098 regulation of appetite

Molecular Function

GO:0004993 G protein-coupled serotonin receptor activity

Cellular Component

GO:0005887 integral component of plasma membrane

Contributing signatures

Signatures from InterPro member databases are used to construct an entry.