RESUMEN
By using a fluorescent 3-metoxybenzatrone probe the binding of the phenothiazine series drugs (chlorpromazine, triftazine, aethaperazine) with phospholipid vesicles--liposomes, was investigated. Cholesterol is shown not to affect the binding of these drugs with liposomes. The surface charge of liposomes influences only the combination with the chlorpromazine membranes. With a higher positive charge of the membranes the binding of chlorpromazine diminishes in force.
Asunto(s)
Antipsicóticos/metabolismo , Liposomas/metabolismo , Proteínas de la Membrana/metabolismo , Animales , Embrión de Pollo , Clorpromazina/metabolismo , Colesterol/metabolismo , Colorantes Fluorescentes , Ácidos Linoleicos/metabolismo , Liposomas/aislamiento & purificación , Perfenazina/metabolismo , Fosfolípidos/aislamiento & purificación , Unión Proteica/efectos de los fármacos , Relación Estructura-Actividad , Propiedades de Superficie , Trifluoperazina/metabolismoRESUMEN
Binding of chlorpromazine, etaperazine and triftazine with model phospholipid membranes was investigated by using a 3-methoxybenzanthrone (MBA) fluorescent probe. All these preparations interacted with the membranes, this being registered by the MBA fluorescence extinction. The phenothiazine molecules bound with the membrane are localized in its superficial layer and extinguish the MBA fluorescence in different ways. The chlorpromazine binding was heterogenous and there are, apparently, 2 different ways of its molecules combination with the membranes. The effective extinction of MBA by phenothiazine increased in the following order: chlorpromazine, etaperazine, triftazine.