Comparison of the beta-adrenoceptor effects of soterenol and its 3-hydroxy, 4-sulphonamido isomer (MJ6987-1) in isolated tissues from the guninea-pig.
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.
D000318:Adrenergic beta-Agonists; D000818:Animals; D002415:Cats; D004983:Ethanolamines / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D007536:Isomerism; D009119:Muscle Contraction / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D013045:Species Specificity; D014590:Uterine Contraction / Q000187:drug effects
D000318:Adrenergic beta-Agonists; D004983:Ethanolamines