β-Adrenergic receptors: Solubilization of (-)[3 H]alprenolol binding sites from frog erythrocyte membranes

Published

Journal Article

The β-adrenergic receptors ((-)[3H]alprenolol binding sites) present in a purified preparation of frog erythrocyte membranes have been solubilized with digitonin and assayed by equilibrium dialysis with (-)[3H]alprenolol. At a concentration of 0.5-1% the detergent solubilizes about 80% of the receptor binding activity. The soluble receptor sites are not sedimented at centrifugal forces up to 105,000 xg for two hours, pass freely through Millipore filters of 0.22 μ pore size and fractionate on Sepharose 6B gel with an apparent molecular weight of 130-150,000 in the presence of digitonin. The soluble receptor sites retain all of the binding characteristics of the membrane-bound receptors. β-adrenergic agonists and antagonists compete with (-)[3H]alprenolol for occupancy of the soluble sites with affinities which are directly related to their β-adrenergic potency on membrane-bound adenylate cyclase. © 1976.

Full Text

Duke Authors

Cited Authors

  • Caron, MG; Lefkowitz, RJ

Published Date

  • January 26, 1976

Published In

Volume / Issue

  • 68 / 2

Start / End Page

  • 315 - 322

Electronic International Standard Serial Number (EISSN)

  • 1090-2104

International Standard Serial Number (ISSN)

  • 0006-291X

Digital Object Identifier (DOI)

  • 10.1016/0006-291X(76)91145-1

Citation Source

  • Scopus