Structure-activity relationship studies of derivatives of aminotetralins and open chain analogs in relation to beta and alpha-adrenoceptor agonist activities.

Some derivatives of aminotetralins and their open chain analogs were tested for their ability to alter blood pressure and heart rate in anesthetized cats with both vagi nerves sectioned and their ability to relax tracheal smooth muscle of guinea-pigs. TL-257 and JOD-213, tertiary amines, produced weak alpha-adrenoceptor stimulating activity while JOD-176 and JOD-211, secondary amines, showed beta-adrenoceptor stimulating activity. Another compounds, M-8, an aminotetralin that is a secondary amine, produced alpha and beta adrenoceptor stimulating activity. The beta-adrenoceptor stimulating activities of M-8 and JOD-176 showed more specificity for beta2-adrenoceptors than for beta1-adrenoceptors.