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Direct analysis of beta-adrenergic receptor subtypes on intact adult ventricular myocytes of the rat

Journal Article · · Circ. Res.; (United States)
beta 1- and beta 2-Adrenergic receptors co-exist in the adult rat ventricle. Radioligand binding and cell purification techniques have been employed to determine the cellular origin of these receptors. The beta-adrenergic antagonist ligand (+/-)-(/sup 125/I) iodocyanopindolol binds to 2 X 10(5) receptors per purified adult rat cardiomyocyte, with a dissociation constant of 70 pM. The subtype-selective antagonists betaxolol (beta 1), practolol (beta 1), and zinterol (beta 2) compete for (/sup 125/I)iodocyanopindolol-binding sites on intact myocytes in monophasic manners with dissociation constants of 46, 845, and 923 nM, respectively. (/sup 125/I)iodocyanopindolol binding to membranes prepared from nonmyocyte elements of rat ventricle occurs with a dissociation constant of 43 pM and a capacity of 88 fmol/mg membrane protein. Computer analysis of competition of (/sup 125/I)iodocyanopindolol binding by betaxolol, practolol, and zinterol in nonmyocyte membranes demonstrates biphasic curves that comprise binding to both beta 1- and beta 2-receptors. These data demonstrate that purified adult ventricular myocytes possess only beta 1-receptors, and that the beta 2-receptors found in rat ventricle are located on nonmyocyte cell types.
Research Organization:
Univ. of California, San Diego, La Jolla
OSTI ID:
5829000
Journal Information:
Circ. Res.; (United States), Journal Name: Circ. Res.; (United States) Vol. 56:1; ISSN CIRUA
Country of Publication:
United States
Language:
English