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  • Title: Selectivity of bunitrolol for beta 1- and beta 2-adrenergic receptors and 5HT1B-receptors: assessment by biphasic Scatchard plots and biphasic displacement curve analysis with 125I-iodocyanopindolol and 3H-CGP12177.
    Author: Tsuchihashi H, Nagotomo T, Imai S.
    Journal: Jpn J Pharmacol; 1989 Jun; 50(2):93-100. PubMed ID: 2570175.
    Abstract:
    The preference by bunitrolol for beta 1- and beta 2-adrenoceptors of the rat brain, heart and/or lung was assessed by the radioligand binding assay method with 125I-iodocyanopindolol (125I-ICYP) or 3H-CGP12177. Scatchard plots of 125I-ICYP binding in the presence of bunitrolol were found to be non-linear. The inhibition constants (Ki) of bunitrolol for high (beta 2-) and low affinity sites (beta 1-) were: 0.42 +/- 0.16 nM for beta 1 and 3.55 +/- 1.61 nM for beta 2 (beta 1 greater than beta 2), respectively. Displacement experiments conducted with the preparations of the rat brain using 125I-ICYP or with the preparations of the rat heart using 3H-CGP12177 yielded Ki values for bunitrolol of 0.53 +/- 0.20 (beta 1) and 2.37 +/- 0.78 (beta 2) nM for 125I-ICYP binding and 2.01 +/- 0.38 (beta 1) and 12.67 +/- 6.54 (beta 2) nM for 3H-CGP12177 binding. In addition, the Ki value for 5HT1B-receptors assessed in displacement experiments conducted with 125I-ICYP in the presence of 30 microM I-metoprolol in the rat brain was 10.54 +/- 5.92 nM. Thus, bunitrolol is a beta 1-selective antagonist.
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