Comparison of the beta-adrenoceptor effects of soterenol and its 3-hydroxy, 4-sulphonamido isomer (MJ6987-1) in isolated tissues from the guninea-pig

Clinical and Experimental Pharmacology & Physiology
G S KehC Raper

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.

Citations

Apr 1, 1976·The Journal of Pharmacy and Pharmacology·W C Bowman, C Raper
Jul 1, 1977·Clinical and Experimental Pharmacology & Physiology·K Bohmer, C Raper
Nov 1, 1975·Clinical and Experimental Pharmacology & Physiology·S R O'Donnell, J C Wanstall
Feb 1, 1970·The Journal of Pharmacy and Pharmacology·J B Farmer, G P Levy
Aug 24, 1968·Nature·D HartleyA C Ritchie
May 1, 1967·Journal of Medicinal Chemistry·A A LarsenP M Lish

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