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

D. 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 to 30 nM. Binding is stereoselective with (-) norepinephrine displaying about twenty times greater affinity that (+) 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 to 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)527-534
Number of pages8
JournalLife Sciences
Volume20
Issue number3
StatePublished - 1977

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Epinephrine
Brain
Norepinephrine
Membranes
Catecholamines
Phenoxybenzamine
Phentolamine
Isoproterenol
Propranolol
Cerebral Cortex
Labels
Binding Sites
Tissue

ASJC Scopus subject areas

  • Pharmacology

Cite this

[3H]Epinephrine and [3H]norepinephrine binding to α noradrenergic receptors in calf brain membranes. / U'Prichard, D. C.; Snyder, Solomon H.

In: Life Sciences, Vol. 20, No. 3, 1977, p. 527-534.

Research output: Contribution to journalArticle

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AB - (±) [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 to 30 nM. Binding is stereoselective with (-) norepinephrine displaying about twenty times greater affinity that (+) 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 to 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.

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