title: Rilmenidine selectivity for imidazoline receptors in human brain.
abstract: The selectivity of three centrally acting antihypertensive agents for the medullary imidazoline-preferring receptors (IPR) versus cortical alpha-adrenoceptors was investigated in human brain. [3H]Clonidine binding was studied in various membrane preparations. Competition experiments were performed. Cortical membrane preparations were used as they mainly contained classical alpha-adrenoceptors whereas medullary membrane preparations from the nucleus reticularis lateralis contained only IPR insensitive to catecholamines. Rilmenidine, a new antihypertensive agent, appeared 2.5 and 3.5 times more selective than clonidine and guanfacine, respectively, for medullary IPR sites than for cortical alpha-adrenoceptors, thus providing a possible explanation for the low sedative effects of this new molecule.
authors.affiliation: Laboratoire de Pharmacologie Cardiovasculaire et Rénale, CNRS URA 589, Faculté de Médecine, Université Louis Pasteur, Strasbourg, France.
authors.forename: G
authors.initials: G
authors.lastname: Bricca
authors.forename: M
authors.initials: M
authors.lastname: Dontenwill
authors.forename: A
authors.initials: A
authors.lastname: Molines
authors.forename: J
authors.initials: J
authors.lastname: Feldman
authors.forename: E
authors.initials: E
authors.lastname: Tibirica
authors.forename: A
authors.initials: A
authors.lastname: Belcourt
authors.forename: P
authors.initials: P
authors.lastname: Bousquet
mesh_terms: D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D054755:Imidazoline Receptors; D066298:In Vitro Techniques; D009419:Nerve Tissue Proteins / Q000378:metabolism; D010080:Oxazoles / Q000494:pharmacology*; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism; D000077769:Rilmenidine
chemical_list: D000316:Adrenergic alpha-Agonists; D054755:Imidazoline Receptors; D009419:Nerve Tissue Proteins; D010080:Oxazoles; D011955:Receptors, Drug; D000077769:Rilmenidine