Relationship between the (--)-[3H]-dihydroalprenolol binding to beta-adrenoceptors and transmembrane 86Rb efflux of the BC3H1 nonfusing muscle cell line

British Journal of Pharmacology
J P Mauger, M Worcel

Abstract

1 We have studied the binding properties of the beta-adrenoceptor antagonist [3H]-dihydroalprenolol ([3H]-DHA) on a membrane preparation of the non-fusing muscle cells BC3H1. 2 [3H]-DHA appears to bind to two classes of sites. The first site has a high affinity (KD = 0.53 nM) and a low capcity (Bmax = 58 fmol/mg of protein). The second site has a low affinity (KD = 110 nM) and a high capacity (Bmax = 1100 fmol/mg of protein). 3 The pharmacological properties of the high affinity low capacity site correspond to the known properties of the beta 2-adrenoceptors since the agonists inhibit [3H]-DHA binding following the series isoprenaline greater than adrenaline greater than noradrenaline greater than phenylephrine and the antagonists following the series alprenolol congruent to propranolol greater than butoxamine greater than practolol greater than phentolamine. 4 The binding properties of the beta-adrenoceptors were correlated with the effect of beta-adrenoceptor agonists and antagonists on 86Rb efflux rate from BC3H1 Cells. 5 There is very good correlation between the dissociation constants obtained by inhibition of [3H]-DHA binding by the antagonists alprenolol and propranolol, and the inhibition constants calculated from their...Continue Reading

References

Jan 1, 1977·Annual Review of Pharmacology and Toxicology·B B WolfeP B Molinoff
Sep 1, 1978·British Journal of Pharmacology·J P MaugerM Worcel
Apr 13, 1976·Biochimica Et Biophysica Acta·R J LefkowitzM G Caron
May 1, 1974·The Journal of Cell Biology·D SchubertS Heinemann
Jan 1, 1968·British Journal of Pharmacology and Chemotherapy·D Dunlop, R G Shanks
Feb 15, 1963·Proceedings of the National Academy of Sciences of the United States of America·M VOGT, R DULBECCO
Sep 1, 1947·British Journal of Pharmacology and Chemotherapy·H O SCHILD

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Citations

Jan 1, 1984·Journal of Receptor Research·F SladeczekJ Bockaert

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