[3H]epinephrine and [3H]norepinephrine binding to α-noradrenergic receptors in calf brain membranes

David C. U'Prichard, Solomon H. Snyder

Research output: Contribution to journalArticle

Abstract

(±)-[3H]Epinephrine and (-)-[3H]norepinephrine bind saturably to calf cerebral cortex membranes under appropriate incubation conditions in a fashion indicating that they label α-noradrenergic receptors. Binding of the two [3H]catecholamines is saturable with dissociation constants of 20-30 nM. Binding is stereoselective with (-)-norepinephrine displaying about twenty times greater affinity than (+)-norepinephrine. The relative potencies of catecholamines in competing for these binding sites parallels their relative pharmacologic effects at α-noradrenergic receptors in numerous tissues. Thus, (-)-epinephrine is 2-3 times more potent than (-)-norepinephrine and 500 times more potent than (-)-isoproterenol. Binding is inhibited by low concentrations of the α-antagonists phentolamine and phenoxybenzamine but not by the β-antagonist propranolol.

Original languageEnglish (US)
Pages (from-to)527-533
Number of pages7
JournalLife Sciences
Volume20
Issue number3
DOIs
StatePublished - Feb 1 1977

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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