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3351 15551 Ensembl ENSG00000135312 ENSMUSG00000049511 UniProt P28222 P28334 RefSeq (mRNA) NM_000863 NM_010482 RefSeq (protein) NP_000854 NP_034612 Location (UCSC) Chr 6: 77.46 – 77.46 Mb Chr 9: 81.51 – 81.52 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse 5-hydroxytryptamine receptor 1B also known as the 5-HT 1B receptor is a protein that in humans is encoded by the HTR1B gene ...
The 5-HT 1 receptors are a subfamily of the 5-HT serotonin receptors that bind to the endogenous neurotransmitter serotonin (also known as 5-hydroxytryptamine, or 5-HT). [1] The 5-HT 1 subfamily consists of five G protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including 5-HT 1A, 5-HT 1B, 5-HT 1D, 5-HT 1E, and 5-HT 1F. [2]
The 5-HT 1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation. 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems.
In addition to being 5-HT 1B agonists, triptans (i.e. sumatriptan, almotriptan, zolmitriptan, naratriptan, eletriptan, frovatriptan and rizatriptan) are also agonists at the 5-HT 1D receptor, which contributes to their antimigraine effect caused by vasoconstriction of blood vessels in the brain. The same is true for ergotamine.
5-HT receptors are all G-protein coupled receptors (GPCR) except for 5-HT 3 which is a ligand gated ion channel. The receptors that have been found to be involved in migraine are 5-HT 1B, 5-HT 1D and 5-HT 1F receptors. 5-HT 1B are found in meningeal arteries, agonism of 5-HT 1B causes vasoconstriction in cranial nerves
Meloxicam/rizatriptan, sold under the brand name Symbravo, is a fixed-dose combination medication used for the treatment of migraine. [1] It is a combination of meloxicam, a nonsteroidal anti-inflammatory medication; and rizatriptan (as rizatriptan benzoate), a serotonin (5-HT) 1B/1D receptor agonist (). [1]
GR-55562 is a selective serotonin 5-HT 1B and 5-HT 1D receptor antagonist. [1] It is one of several selective serotonin 5-HT 1B receptor antagonists used in scientific research. [2] [3] The drug is a silent antagonist of the serotonin 5-HT 1B receptor, unlike the related agent GR-127935.
5-(Nonyloxy)tryptamine (5-NOT) is a tryptamine derivative which acts as a selective agonist at the 5-HT 1B receptor.Increasing the O-alkoxy chain length in this series gives generally increasing potency and selectivity for 5-HT 1B, with highest activity found for the nonyloxy derivative, having a 5-HT 1B binding affinity of 1.0 nM, and around 300-fold selectivity over the related 5-HT 1A receptor.