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Description: Nebivolol (also known as R-65824) potently and selectively inhibits beta1-adrenoceptor with IC50 of 0.8 NM. Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50). Nebivolol displays beta1-adrenoceptor selectivity with the Ki(beta2)/Ki(beta1) value of 40.7 judged by competition experiments to 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kibeta2) or ICI 118.551 (50 nM, Kibeta1).
References: Mol Pharmacol. 1988 Dec; 34(6):843-51; Circ J. 2008 Apr; 72(4):660-70.
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