Uptake of radioligands by rat heart and lung in vivo: CGP 12177 does and CGP 26505 does not reflect binding to beta-adrenoceptors

European Journal of Pharmacology
A van WaardeK I Lie

Abstract

The biodistribution of (-)-4-(3-t-butylamino-2-hydroxypropoxy)-[5,7-3H-benzimidazol-2-one (CGP12177, a non-selective beta-adrenoceptor antagonist) and 1-[2-(3-carbamoyl-4-hydroxy)-(5-3H-phenoxy)]-2-propanol methanesulfonate, (CGP26505, a beta 1-adrenoceptor antagonist) was studied in rats pretreated with various alpha- and beta-adrenoceptor blocking drugs (5 min before 3H injection, in dosages at which the drugs demonstrated the expected selectivity). Cardiac and pulmonary radioactivity were measured after 10 min, when specific binding was maximal. Uptake of [3H]CGP12177 was linked to binding to beta-adrenoceptors since it was not affected by prazosin or yohimbine, and was equally well inhibited by propranolol, unlabelled CGP12177 and isoprenaline. Moreover, atenolol and CGP20712A inhibited [3H]CGP12177 uptake in heart (predominantly beta 1-adrenoceptors) more potently than ICI 118,551, while in lungs (predominantly beta 2-adrenoceptors) ICI 118,551 was more potent than atenolol or CGP20712A. In contrast, [3H]CGP26505 uptake in the target organs was equally effectively inhibited by propranolol and ICI 118,551, and significantly lowered by alpha-adrenoceptor antagonists. We conclude that [11C]CGP12177, but not [11C]CGP2605 will ...Continue Reading

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Citations

Nov 28, 2012·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·James T Thackeray, Frank M Bengel
May 7, 1998·European Journal of Pharmacology·A van WaardeW Vaalburg
Jun 9, 2000·Kidney International·G GabriëlsM Steinhausen
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Dec 1, 1996·Journal of Autonomic Pharmacology·R A NicholasT K Harden
Dec 1, 1996·Journal of Autonomic Pharmacology·G Lambrecht
May 23, 1998·Annual Review of Pharmacology and Toxicology·D K Rohrer, B K Kobilka
May 12, 1998·The American Journal of Physiology·D K RohrerD Bernstein
Mar 23, 2017·Current Cardiology Reports·Nabil E Boutagy, Albert J Sinusas

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