PMID: 2872766Mar 1, 1986

Partial agonism and functional selectivity: a study on beta-adrenoceptor mediated effects in tracheal, cardiac and skeletal muscle

Acta Pharmacologica Et Toxicologica
B WaldeckE Widmark

Abstract

Colterol, procaterol, sulfonterol, terbutaline and three monophenolic derivatives of terbutaline were examined with respect to their ability to react in vitro on beta-adrenoceptors in tissues isolated from guinea-pig. The effects measured were a) relaxation of the tracheal smooth muscle (mostly beta 2), b) depression of subtetanic contractions of the soleus muscle (beta 2), and c) increase in the force of the papillary muscle of the left ventricle (beta 1). Antagonistic effects were measured against isoprenaline as an agonist. The compounds studied showed a wide variation in selectivity, potency and intrinsic activity. All agonists showed a pronounced beta 2-selectivity, in general characterized by a higher intrinsic activity at beta 2- than at beta 1-adrenoceptors, while differences in affinity, as judged from the pA2-values were small. Partial agonists, such as sulfonterol, which did not cause a complete relaxation of a moderately contracted tracheal muscle, produced identical concentration-response curves from the trachea and soleus muscle. It is concluded that partial agonism at beta 1-adrenoceptors is an important factor for functional selectivity of beta 2-adrenoceptor agonists. On the other hand there seems to be no usef...Continue Reading

References

Sep 1, 1977·The Journal of Pharmacy and Pharmacology·B Waldeck
Jan 1, 1969·British Journal of Pharmacology·V A CullumG P Levy
Oct 1, 1982·Acta Pharmacologica Et Toxicologica·P AnderssonB Waldeck
Dec 1, 1983·The Journal of Pharmacy and Pharmacology·L H Johansson, H Persson
Dec 1, 1982·Journal of Autonomic Pharmacology·R R Ruffolo
Feb 1, 1980·Acta Pharmacologica Et Toxicologica·E Holmberg, B Waldeck
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

Citations

Jun 1, 1997·Journal of Veterinary Pharmacology and Therapeutics·K TörnekeL E Appelgren
Jul 9, 2002·Clinical and Experimental Pharmacology & Physiology·Hiroshi MizutaniKenichi Yamaki
Mar 1, 1990·Pharmacology & Toxicology·L H JohanssonE Rosengren
Oct 1, 1992·Pharmacology & Toxicology·A B JeppssonB Waldeck
Sep 1, 1991·Journal of Veterinary Pharmacology and Therapeutics·C Ingvast-Larsson

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