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Irreversible binding of the fluorescent beta-adrenoceptor probes alprenolol-NBD and pindolol-NBD to specific and non-specific binding sites

Rademaker, B.; Kramer, K.; Bast, A.; Timmerman, H.

Research Communications in Chemical Pathology and Pharmacology 60(2): 147-159

1988

ISSN/ISBN: 0034-5164
PMID: 2839876
Document Number: 323293
The fluorescent 4-nitrobenzo-2-oxa-1,3-diazolyl (NBD) derivatives of alprenolol and pindolol bind irreversible to beta-adrenoceptors and non-receptor binding sites. This was established in functional experiments on the guinea pig right atrium and trachea smooth muscle, and by radioligand binding assay of beta-adrenoceptors on Chang liver cells in culture. The pD2'-values of alprenolol-NBD and pindolol-NBD for the beta-adrenoceptors on the right atrium were: 8.3 +/- 0.1 and 8.5 +/- 0.1; on the tracheal smooth muscle strip: 8.2 +/- 0.1 and 8.8 +/- 0.1; and its pKd on Chang liver cells: 8.5 +/- 0.1 and 8.9 +/- 0.1 respectively. The results indicated that no selectivity for the beta-adrenoceptor subtypes was introduced by the addition of NBD. The irreversible binding characteristic to beta-adrenoceptors and non-receptor binding sites of the fluorescent NBD derivatives of alprenolol and pindolol makes these drugs unsuitable to label beta-adrenoceptors specifically. As the irreversible binding is introduced by the coupling of the drug with NBD, it is concluded that NBD derivatives of beta-adrenoceptor antagonists are not suitable to visualize the two-dimensional motion of beta-adrenoceptors during challenge with agonists.

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Dziarski, R. 1992: Specific endotoxic lipopolysaccharide-binding receptors on murine splenocytes: III. Binding specificity and characterization Journal of Immunology 148(5): 1590-1591
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