Molecular biology of 5-HT receptors

The receptors through which serotonin (5-hydroxytryptamine, 5-HT) produces its effects have been the subject of intense investigation, initially using both in vivo and in vitro pharmacological methods, and later radioligand binding. These approaches allowed a preliminary classification of 5-HT receptors, but the identification on subtypes was limited by the selectivity on the available agonists and antagonists. Bradley et al. (1986) distinguished three main classes of 5-HT receptors: 5-HT 1 , 5-HT 2 and 5-HT 3 . 5-HT 3 receptors were activated by the selective agonist 2-methyl-5-HT and blocked by selective antagonists such as (-)cocaine, MDL72222 and tropisetron (ICS 205-930)