RESUMEN

A series of 2-(arylamino)imidazoles was synthesized and evaluated for activity at alpha 1- and alpha 2-adrenoceptors. This class of agents has been shown to have potent and selective agonist activity at the alpha 2-adrenoceptors. The most potent member of this class, 2-[(5-methyl-1,4-benzodioxan-6yl)amino]imidazole, proved efficacious for the reduction of intraocular pressure upon topical administration and for the reduction of blood pressure upon intravenous administration. During the course of our studies, we developed a new reagent that allowed rapid assembly of the target compounds. This reagent, N-(2,2-diethoxyethyl)carbodiimide, was convenient to prepare and was stable under low-temperature storage conditions.

Asunto(s)

Agonistas de Receptores Adrenérgicos alfa 2 , Imidazoles/química , Animales , Barrera Hematoencefálica/efectos de los fármacos , Tartrato de Brimonidina , Imidazoles/farmacología , Presión Intraocular/efectos de los fármacos , Macaca fascicularis , Quinoxalinas/química , Quinoxalinas/farmacología , Conejos

Asunto(s)

Agonistas alfa-Adrenérgicos/síntesis química , Compuestos Bicíclicos con Puentes/síntesis química , Heptanos/síntesis química , Receptores de Droga/metabolismo , Agonistas alfa-Adrenérgicos/metabolismo , Agonistas alfa-Adrenérgicos/farmacología , Animales , Sitios de Unión , Presión Sanguínea/efectos de los fármacos , Compuestos Bicíclicos con Puentes/metabolismo , Compuestos Bicíclicos con Puentes/farmacología , Células CHO , Cricetinae , Heptanos/metabolismo , Heptanos/farmacología , Humanos , Receptores de Imidazolina , Macaca fascicularis , Ratas