3H]R-terazosin binds selectively to alpha1-adrenoceptors over alpha2-adrenoceptors - comparison with racemic [3H]terazosin and [3H]prazosin

European Journal of Pharmacology
L M IrelandJ F Kerwin

Abstract

Most tissue sources for adrenoceptors contain a mixed population of alpha1- and/or alpha2-adrenoceptor subtypes; thus studies using non-specific radioligands are complicated by receptor heterogeneity. The examination of alpha1-adrenoceptor radioligand binding by radiolabeled terazosin and its enantiomers was simplified by using mouse fibroblast cells, which are thymidine kinase mutant (LTK-), transfected with cloned alpha1a-, alpha1b-, and alpha1d-adrenoceptor subtypes. [3H]Terazosin and its enantiomers were equipotent at the alpha1b-adrenoceptor. [3H]R-Terazosin was significantly less potent than [3H]terazosin and [3H]S-terazosin at the alpha1a- and the alpha1d-adrenoceptors. Using tissue derived alpha-adrenoceptors prepared in cold 25 mM glycyl-glycine buffer, [3H]prazosin, [3H]terazosin and [3H]S-terazosin bound to two sites in the rat neonatal lung preparation consistent with the presence of both alpha1- and alpha2B-adrenoceptors. The relative binding potencies of these radioligands at these two sites correlated with low affinity binding to the alpha2B-adrenoceptor and high affinity binding to an alpha1-adrenoceptor. [3H]R-Terazosin, on the other hand, bound to a single site in the rat neonatal lung membrane preparation, mo...Continue Reading

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Citations

Oct 12, 2007·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Michael HultströmA Erik G Persson
Aug 2, 2003·Clinical and Experimental Pharmacology & Physiology·Erika I BoesenWarwick P Anderson
Oct 27, 2005·The Journal of Pharmacology and Experimental Therapeutics·Qian ChenHui-Lin Pan
Jul 31, 1999·General Pharmacology·G P McCaffertyJ P Hieble
Dec 3, 2003·Brain Research·M Laura CuffiJavier Forn

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