5-Hydroxytryptamine 7 receptor (IPR001069)

Short name: 5HT_7_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-HT7 receptor has been shown to positively modulate cAMP formation [PMID: 8226867, PMID: 8398139, PMID: 9808674] and activate the mitogen-activated protein kinase, ERK, in primary neuronal cultures [PMID: 1166122]. The receptor is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels [PMID: 8226867]. It has an extensive vascular distribution [PMID: 10374714] and is responsible for the prominent, persistent vasodilator response to 5-HT7 in anaesthetised animals [PMID: 7984266]. 5-HT7 receptors are involved in thermoregulation [PMID: 12763096, PMID: 15033384] circadian rhythm [PMID: 14654097], learning and memory, and sleep [PMID: 12812993]. This receptor has been a drug development target for the treatment of several clinical disorders [PMID: 18301795]. Atypical antipsychotics, e.g. clozapine, risperidone and antidepressants, have high affinity for the 5-HT7 receptor [PMID: 7908055] and it has been speculated that the 5-HT7 receptor may be involved in mood regulation, suggesting that it may be a useful target in the treatment of depression [PMID: 15559250].

GO terms

Biological Process

GO:0007186 G-protein coupled receptor signaling pathway
GO:0007268 chemical synaptic transmission
GO:0007623 circadian rhythm
GO:0006939 smooth muscle contraction
GO:0042310 vasoconstriction

Molecular Function

GO:0004993 G-protein coupled serotonin receptor activity

Cellular Component

GO:0016021 integral component of membrane

Contributing signatures

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