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5-hydroxytryptamine receptor 7 isoform a (5-HT7A) (5-HT7A)

Target
5-HT7A
Molecular classification
G protein-coupled receptor [1], Receptor [2]
01

Overview

The 5-hydroxytryptamine receptor 7 isoform a (5-HT7A) is a specific splice variant of the 5-HT7 receptor, a G protein-coupled receptor (GPCR) that stimulates adenylyl cyclase via the Gs signaling pathway to increase intracellular cAMP [1, 2]. It is the most prevalent isoform in human tissues and is widely expressed in the central nervous system, particularly in the hypothalamus, thalamus, and hippocampus [1, 3]. In these regions, the receptor plays a critical role in regulating circadian rhythms, sleep-wake cycles, and cognitive processes such as learning and memory [2, 4]. Beyond the brain, the 5-HT7 receptor is involved in smooth muscle relaxation within the gastrointestinal tract and vasculature [2, 5]. Clinically, it is a significant target for neuropsychiatric conditions; several atypical antipsychotics and antidepressants, including lurasidone and vortioxetine, act as high-affinity antagonists or modulators at this receptor to treat depression and cognitive impairment [4, 5].

Other names
HTR7Serotonin receptor 75-HT75-hydroxytryptamine receptor 7 isoform a5-HT7R
02

Mechanism of action

Modulation of Gs-protein signaling to regulate intracellular cyclic adenosine monophosphate (cAMP) levels, thereby influencing neuronal excitability and smooth muscle tone [1, 2].

03

Biological functions

Signal transduction [1]Circadian rhythm regulation [3]Thermoregulation [3]Learning and memory [4]Smooth muscle relaxation [2]
04

Disease associations

Major depressive disorder [4]Schizophrenia [4]Circadian rhythm sleep disorders [3]Migraine [2]Irritable bowel syndrome [5]Cognitive impairment [4]
05

Safety considerations

Thermoregulatory dysfunction [3]Alterations in sleep architecture [4]Gastrointestinal motility changes [2]
06

Interacting drugs

Vortioxetine [4]

7 more in the full profile.

07

Biomarkers

Intracellular cAMP levels [1][11C]SB-269970 (PET imaging ligand) [4]

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