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Several drugs that act as 5-HT 4 selective agonists have recently been introduced into use in both scientific research and clinical medicine. Some drugs that act as 5-HT 4 agonists are also active as 5-HT 3 antagonists, such as mosapride, metoclopramide, renzapride, and zacopride, and so these compounds cannot be considered highly selective.
RS-127445, also known as MT-500, is a drug which acts as a potent and selective antagonist at the serotonin 5-HT 2B receptor, with around 1,000-fold selectivity over the closely related 5-HT 2A and 5-HT 2C receptors. [1] The role of the 5-HT 2B receptor in the body is still poorly understood, and RS-127445 has been a useful tool in unravelling ...
4-HT is a potent agonist of the serotonin 5-HT 2A receptor similarly to psilocin (EC 50 Tooltip half-maximal effective concentration = 38 nM and 21 nM, respectively). [4] It produces serotonergic peripheral effects in animals, [1] [10] shows similar metabolism and metabolic stability to psilocin, [4] and appears to cross the blood–brain barrier and hence is centrally penetrant.
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. [ 1 ] [ 2 ] [ 3 ] They mediate both excitatory and inhibitory neurotransmission .
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]
2-Methyl-5-hydroxytryptamine (2-Methylserotonin, 2-Methyl-5-HT) is a tryptamine derivative closely related to the neurotransmitter serotonin which acts as a moderately selective full agonist at the 5-HT 3 receptor.
15564 Ensembl ENSG00000125631 ENSMUSG00000050534 UniProt n a P31387 RefSeq (mRNA) n/a NM_010483 RefSeq (protein) n/a NP_034613 Location (UCSC) n/a Chr 1: 121.44 – 121.46 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse 5-HT 5B receptor is a 5-HT receptor protein and the gene which encodes it. The protein is found in rodents, but not in humans, because stop codons in the gene's ...
The 5-HT 7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). [5] The 5-HT 7 receptor is coupled to G s (stimulates the production of the intracellular signaling molecule cAMP) [6] [7] and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in ...