Summary
Catecholamine-induced stimulation of adenylyl cyclase in ventricular membranes of kitten and Xenopus laevis was antagonized competitively by carazolol. Apparent equilibrium constants ranging between 100–170 pM were estimated for the β-adrenoceptorcarazolol complex.
References
Arunlakshana, O., Schild, H. O.: Some quantitative uses of drug antagonists. Br. J. Pharmacol. 14, 48–58 (1959)
Carlsson, E., Åblad, B., Brändström, A., Carlsson, B.: Differentiated blockade of the chronotropic effects of various adrenergic stimuli in the cat heart. Life Sci. 11, 953–958 (1972)
Kaumann, A. J.: Some differences between heart β-adrenoceptors of reserpine-pretreated rats (Wistar II) and frogs (Xenopus laevis). Naunyn-Schmiedeberg's Arch. Pharmacol. 297, R49 (1977)
Kaumann, a. J., Birnbaumer, L.: Characteristics of the adrenergic receptor coupled to myocardial adenylyl cyclase: Stereospecificity and determination of apparent affinity constants for β-blockers. J. Biol. Chem. 249, 7874–7885 (1974)
Lee, W. C., Shideman, F. E.: Mechanism of the positive inotropic response to certain ganglionic stimulants. J. Pharmacol. Exp. Ther. 126, 239–249 (1959)
Lemoine, H., Kaumann, A. J.: The affinity of carazolol for myocardial and tracheal β-adrenoceptors activated by (-)-isoprenaline. Naunyn-Schmiedeberg's Arch. Pharmacol. 302, R53 (1978)
Lowry, O. H., Rosebrough, N. J., Farr, A. L., Randall, R. J.: Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193, 265–275 (1951)
Salomon, Y., Londos, C., Rodbell, M.: A highly sensitive adenylate cyclase assay. Anal. Biochem. 58, 541–548 (1974)
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Morris, T.H., Birnbaumer, L. & Kaumann, A.J. High affinity of carazolol for β-adrenoceptors coupled to the adenylyl cyclase in ventricular myocardium of kitten and xenopus laevis . Naunyn-Schmiedeberg's Arch. Pharmacol. 303, 295–297 (1978). https://doi.org/10.1007/BF00498057
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00498057