Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine found in the central nervous system, gastrointestinal tract, and blood with broad physiological functions as a neurotransmitter, in gastric motility, hemostasis, and cardiovascular integrity. Seven subclasses (5-HT 1-7) of serotonin receptors have been identified, a majority of which are members of the seven transmembrane domain-containing G-protein coupled receptor (GPCR) family, and are the target of several anti-depressant drugs. The 5-HT1 subclass consists of five highly homologous receptors that couple via G(i/o) alpha subunits to inhibit adenylyl cyclase activity. The 5-HT1A receptor gene is 99% homologous between human and mouse, and is expressed from an intronless gene with a predicted length of 421 amino acids. 5-HT1A receptor activation is generally inhibitory to cAMP production, but may also stimulate type II adenylyl cyclase activity in a cell-specific manner via release of G(beta/gamma) subunits when coupled to G(i2). 5-HT1A expression in mammals is strongest in CNS limbic pathways that control emotion, including tissue of the hippocampus, dorsal raphé, and septum.
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Regulatory Status |
RUO – Research Use Only |
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