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Target intelligence / Profile preview
Serotonin 5-HT7 Receptor (5-HT7)
- Target
- 5-HT7
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The serotonin 5-HT7 receptor is a G protein-coupled receptor activated by serotonin (5-HT). It is widely expressed in the central nervous system and peripheral tissues, mediating diverse physiological functions including thermoregulation, circadian rhythms, learning, and gastrointestinal motility. It is implicated as a therapeutic target for several disorders, including depression, schizophrenia, irritable bowel syndrome, and circadian rhythm disorders. Activation results in increased cAMP levels. No selective drugs targeting only this subtype are currently approved for clinical use.
- Other names
- Serotonin receptor 7HTR75-hydroxytryptamine receptor 75HT₇Serotonin-X receptorSerotonin-VII receptor
02
Mechanism of action
Activation by serotonin leads to Gs protein activation, increasing intracellular cAMP levels. Antagonists block serotonin binding, preventing cAMP increase.
03
Biological functions
Signal transductionRegulation of body temperatureModulation of circadian rhythmsRegulation of sleep/wake cycleLearning and memory processesSmooth muscle relaxationVasodilationGastrointestinal motility
04
Disease associations
DepressionSchizophreniaSleep disordersCircadian rhythm disordersIrritable bowel syndromeAutism spectrum disordersRett syndromeTriple-negative breast cancer
05
Safety considerations
Lack of highly selective drugs targeting only 5-HT7Potential for off-target effects with non-selective drugsLimited clinical data on selective 5-HT7 modulators
06
Interacting drugs
Antidepressants (some)
2 more in the full profile.
07
Biomarkers
HTR7 expression in triple-negative breast cancer
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