5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the HTR5A gene. Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes.
The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via G<sub>i</sub> and G<sub>o</sub>. This protein has been shown to function in part through the regulation of intracellular Ca<sup>2+</sup> mobilization. The 5-HT<sub>5A</sub> receptor has been shown to be functional in a native expression system.
Rodents have been shown to possess two functional 5-HT<sub>5</sub> receptor subtypes, 5-HT<sub>5A</sub> and 5-HT<sub>5B</sub>, however while humans possess a gene coding for the 5-HT<sub>5B</sub> subtype, its coding sequence is interrupted by stop codons, making the gene non-functional, and so only the 5-HT<sub>5A</sub> subtype is expressed in human brain.
It also appears to serve as a presynaptic serotonin autoreceptor.
The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) has been implicated in a wide range of psychiatric conditions and also has vasoconstrictive and vasodilatory effects.
Few highly selective ligands are commercially available for the 5-HT<sub>5A</sub> receptor, though the field has expanded considerably in recent years. When selective activation of this receptor is desired in scientific research, the non-selective serotonin receptor agonist 5-Carboxamidotryptamine can be used in conjunction with selective antagonists for its other targets (principally 5-HT<sub>1A</sub>, 5-HT<sub>1B</sub>, 5-HT<sub>1D</sub>, and 5-HT<sub>7</sub>). Research in this area is ongoing.