title: The extraction, isolation and purification of an endogenous regulator for the 5-HT2 receptor.
abstract: Early studies indicated that serotonin, a primary transmitter in the central nervous system, may not represent the primary endogenous regulator for the 5-HT2 receptor labeled by [3H]-ketanserin. Instead, an endogenous ligand may be responsible for modulating the [3H]-ketanserin site. Through different isolation and purification procedures, a pronase-sensitive peptide with activity on [3H]-ketanserin binding was identified in the rat brain. This peptide seems specific for the 5-HT2 receptor since it does not displace the binding of [3H]-imipramine or [3H]-mianserin from rat cortical membranes and is able to stimulate PI turnover in a ketanserin sensitive fashion. Given the role of 5-HT2 receptors in the action of antidepressants, this finding may help understand some of the molecular mechanisms involved in antidepressant effect.
authors.affiliation: Clinical Brain Disorders Branch, GCAP, NIMH, NIH, Building 10, CRC 7-3342, 10 Center Dr., Bethesda, MD 20892, United States. apudj@mail.nih.gov
authors.forename: José A
authors.initials: JA
authors.lastname: Apud
mesh_terms: D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D007650:Ketanserin / Q000494:pharmacology; D010455:Peptides / Q000302:isolation & purification* / Q000378:metabolism*; D044348:Receptors, Serotonin, 5-HT2 / Q000737:chemistry / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000494:pharmacology
chemical_list: D010455:Peptides; D044348:Receptors, Serotonin, 5-HT2; D012702:Serotonin Antagonists; D007650:Ketanserin