Biological Activity
Oxprenolol-d7 is intended for use as an internal standard for the quantification of oxprenolol by GC- or LC-MS. Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue).1 It is non-selective and binds to both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively).2 Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively).3,4 Formulations containing oxprenolol have been used to treat hypertension and angina pectoris.5
References
1.Nagatomo, T., Sasaki, M., Tsuchihashi, H., et al.Binding characteristics of 3H-dihydroalprenolol to β-adrenoceptors of rat heart treated with neuraminidaseJpn. J. Pharmacol.33(4)851-857(1983)
2.Abrahamsson, T.The β1- and β2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: A study in the isolated right atrium and uterus of the ratBr. J. Pharmac.87(4)657-664(1986)
3.Moretti-Rojas, I., Ezrailson, E.G., Birnbaumer, L., et al.Serotonergic and adrenergic regulation of skeletal muscle metabolism in the rat. II. The use of [125I]iodolysergic acid diethylamide and [125I]iodopindolol as probes of sarcolemmal receptor function and specificityJ. Biol. Chem.258(20)12499-12508(1983)
4.Langlois, M., Brémont, B., Rousselle, D., et al.Structural analysis by the comparative molecular field analysis method of the affinity of β-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptorsEur. J. Pharmacol.244(1)77-87(1993)
5.Russo, M.E., and Covinsky, J.O.Oxprenolol hydrochloride: Pharmacology, pharmacokinetics, adverse effects and clinical efficacyPharmacotherapy3(2)68-81(1983)
