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QuickView for 5-Hydroxytryptamine 1F receptor (biogroup)
- 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 the 5-HT1F receptors, they are thought to be closely related 5-HT1E receptors. They have a limited distribution in peripheral tissues in human, and have been detected only in the uterus and mesentery. In the CNS, receptor mRNA is present in the cerebral cortex, hippocampus, raphe and spinal cord. Elucidation of the physiological role of 5-HT1F receptors requires development of selective ligands. At present, there are no selective antagonists or agonists. However, the 5-HT1D/5-HTD1B agonist and anti-migraine compound sumatriptan has reasonable affinity. Interestingly, 5-HT1F receptor expression has been detected in the trigeminal ganglia, stimulation of which leads to the plasma extravasation in the dura, a component of neurogenic inflammation thought to be a possible cause of migraine.
- Taxonomy/Path:
- InterPro : Opsin, invertebrate / 5-Hydroxytryptamine 1F receptor
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