4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone: a prejunctional dopamine receptor agonist.

Gallagher, G; Lavanchy, P G; Webster, C A; Wilson, J W; Hieble, J P; DeMarinis, R M

Gallagher, G; Lavanchy, P G; Webster, C A; Wilson, J W; Hieble, J P; DeMarinis, R M.

J Med Chem ; 28(10): 1533-6, 1985 Oct.

Article en En | MEDLINE | ID: mdl-4045928

RESUMEN

4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone (1c) (SK&F 101468) is a potent and selective prejunctional dopamine receptor agonist. It caused a dose-related inhibition of the constrictor response to electrical stimulation in the isolated perfused rabbit ear artery (EC50 = 100 nM), and this response was antagonized by (S)-sulpiride (KB = 7 nM). Compound 1c did not stimulate or block dopamine-sensitive adenylate cyclase and did not produce stimulation of the central nervous system in rats. It was prepared from (2-methyl-3-nitrophenyl)acetic acid in a multistep sequence based on the Reissert indole synthesis.

Asunto(s)

Indoles/farmacología; Receptores Dopaminérgicos/efectos de los fármacos; Animales; Fenómenos Químicos; Química; Indoles/metabolismo; Conejos; Sistema Vasomotor/efectos de los fármacos

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores Dopaminérgicos / Indoles Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1985 Tipo del documento: Article Pais de publicación: Estados Unidos

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