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5‐Hydroxytryptamine Receptors
Author(s) -
Peroutka Stephen J.
Publication year - 1993
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1993.tb03166.x
Subject(s) - receptor , methysergide , class c gpcr , antagonism , 5 ht receptor , rhodopsin like receptors , g protein coupled receptor , 5 ht1 receptor , biology , serotonin , serotonin antagonists , chemistry , ion channel , pharmacology , biochemistry , metabotropic receptor , agonist
5‐Hydroxytryptamine (5‐HT) receptors consist of at least three distinct types of molecular structures (Table 1): guanine nucleotide binding protein (G protein)‐coupled receptors, ligand‐gated ion channels, and transporters. Prior to the introduction of molecular biological techniques, the classification of 5‐HT receptors was based predominantly on the pharmacological properties of the receptors. For example, “5‐HT 1 ” receptors were defined as membrane binding sites that displayed nanomolar affinity for [ 3 H]5‐HT (Peroutka and Snyder, 1979). Subsequently, Bradley et al. (1986) defined “5‐HT 1‐like ” receptors by their susceptibility to antagonism by methiothepin and/or methysergide, resistance to antagonism by 5‐HT 2 antagonists, and potent agonism by 5‐carboxamidotryptamine (5‐CT). Thus, these classification systems are dependent upon the availability of selective pharmacological agents.