Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular myocardium and lung

Circulation Research
A S ManalanA M Watanabe


[3H](+/-)Carazolol, a newly available beta-adrenergic receptor antagonist, can be used to characterize beta-adrenergic receptor subtypes present in membrane vesicles derived from canine ventricular myocardium and canine lung. [3H](+/-)Carazolol binding is saturable, of high affinity, and is displaceable by beta-adrenergic agents in accordance with their known pharmacological potencies. The interaction of carazolol with beta-adrenergic receptors is stereospecific; the (-) stereoisomer demonstrates greater potency than the (+) stereoisomer. Kinetic analysis of [3H](+/-)carazolol interaction with beta-adrenergic receptors suggests that presence of two phases of interaction, consistent with initial rapidly reversible "low" affinity association of ligand with receptor, followed by isomerization to form a high affinity, slowly reversible complex. Through use of a [3H](+/-)carazolol binding assay based on the high affinity complex, pharmacological specificities of beta-adrenergic receptor populations of canine myocardium and lung were quantified. Analysis using computer-assisted techniques suggests a beta 1/beta 2 receptor ratio of approximately 85%/15% for canine myocardium and 5%/95% for canine lung. In the absence of added guanine ...Continue Reading


Sep 1, 1986·Naunyn-Schmiedeberg's Archives of Pharmacology·M FreissmuthW Schütz
Mar 1, 1982·Naunyn-Schmiedeberg's Archives of Pharmacology·D HoyerR Berthold
Jul 1, 1984·Naunyn-Schmiedeberg's Archives of Pharmacology·R R RuffoloJ S Horng
Aug 15, 1985·European Journal of Pharmacology·X L WangO E Brodde
Apr 16, 1986·European Journal of Pharmacology·H J SchliepG Haeusler
Jan 1, 1988·Progress in Biophysics and Molecular Biology·H C Hartzell
Oct 1, 1984·Journal of Molecular and Cellular Cardiology·J H ImC E Rackley
Aug 23, 2002·Journal of Psychiatric Research·Paul J AmbrosiniNick Haslam
Jan 1, 1983·Journal of the American College of Cardiology·A M Watanabe
Oct 1, 2003·Clinical Positron Imaging : Official Journal of the Institute for Clinical P.E.T·Philip H. ElsingaWillem Vaalburg
Jun 26, 2001·British Journal of Clinical Pharmacology·A H AbdelmawlaC M Bradshaw
Apr 8, 2010·SAR and QSAR in Environmental Research·V N NovoseletskyR G Efremov
Dec 1, 1990·Journal of Veterinary Pharmacology and Therapeutics·F KadirJ H Verheijden
May 1, 1982·Clinical and Experimental Pharmacology & Physiology·A J Man in 't Veld, M A Schalekamp
Nov 1, 1992·Clinical and Experimental Pharmacology & Physiology·A HoeyC Sernia
Dec 1, 1985·The Journal of Clinical Investigation·D E VatnerC J Homcy
Mar 1, 1993·The Journal of Clinical Investigation·K KiuchiD E Vatner
Jan 1, 1984·European Journal of Clinical Pharmacology·J W LammersC L van Herwaarden
Apr 8, 2014·Journal of Pharmacological and Toxicological Methods·Geoffrey TruchettiSimon Authier
Jul 14, 1986·Life Sciences·L G MeggsA I Goodman
Dec 1, 1987·Journal of Clinical Pharmacy and Therapeutics·J V Okopski
Feb 1, 1983·Archives of Biochemistry and Biophysics·S A Morris, J P Bilezikian
Feb 28, 2020·Chirality·Vinod Kumar Vashistha, Anuj Kumar
Aug 1, 1983·Biological Reviews of the Cambridge Philosophical Society·S C Makrides
Sep 1, 1986·British Journal of Clinical Pharmacology·G LeopoldH Wiemann
Jan 1, 1982·British Journal of Clinical Pharmacology·A J Man in't VeldM A Schalekamp
Sep 1, 1984·British Journal of Clinical Pharmacology·A E TattersfieldR J Bacon
Nov 1, 1986·Journal of Clinical Pharmacology·G LeopoldK U Bühring
Mar 28, 1998·British Journal of Clinical Pharmacology·A H AbdelmawlaC M Bradshaw
Sep 28, 2017·Scientific Reports·Gyuzel Y MitronovaStefan W Hell

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