| Primary Identifier | IPR027425 | Type | Family |
| Short Name | 5HT1E_rcpt |
| description | 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 []. 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 [], all 5-HT receptors are members of the rhodopsin-like G protein-coupled receptor family [], and they activate an intracellular second messenger cascade to produce their responses. The 5-HT1 receptors are a subfamily of 5-HT receptors that were originally classified according to their inhibition of adenylyl cyclase, degree of sequence similarity and their overlapping pharmacological specificities. The subfamily is comprised of five different receptors 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT1F, and they can couple to Gi/Go and mediate inhibitory neurotransmission, although signalling via other transduction systems are known. One of the 5-HT1 receptors, the 5-HT1E receptor, is yet to achieve receptor status from the International Union of Basic and Clinical Pharmacology (IUPHAR), since a robust response mediated via the protein has not been reported in the literature.This entry represents 5-HT1E receptor. It was first identified in the frontal cortex of the human brain. The exact function of the receptor is presently unknown, due to the lack of selective ligands []. It is thought to be negatively linked to adenylyl cyclase in recombinant cell systems and may have an important evolutionary role in humans []. It is hypothesized that the 5-HT1E receptor is involved in the regulation of memory, due to the high abundance of receptors in the frontal cortex, hippocampus, and olfactory bulb [, ], all of which are regions of the brain integral to memory regulation []. The 5-HT1E receptor, like the 5-HT1F receptor, has high affinity for 5-HT and low affinity for 5-carboxyamidotryptaine and mesulergine []. However, the 5-HT1E receptor has a relatively low affinity for sumatriptan, which sets it apart from the 5-HT1F receptor []. |
