Comparison of the ?-Adrenoceptor Effects of Soterenol and its 3-Hydroxy, 4-Sulphonamido Isomer (MJ6987-1) in Isolated Tissues from the Guinea-Pig

Abstract

1. Soterenol and its 3-hydroxy, 4-methanesulphonamido isomer (MJ6987-1) were compared with isoprenaline for beta-adrenoceptor mediated effects in guinea-pig atrial, tracheal, uterine and ileal preparations. In addition, MJ6987-1 was tested for its effects in the atria of cats, rabbits and rats. 2. Soterenol had a lower intrinsic activity and was approximately two to six times less active than isoprenaline in all preparations. 3. MJ6987-1 was a full agonist, being some 30--200 times less active than isoprenaline at beta 1-receptor sites and greater than 3000 times less active in preparations where beta 2-receptor activation was involved. 4. Change in the position of the ring substituents in soterenol leads to the production of beta 1-receptor selective agonist.