A simple, sensitive and specific radioreceptor assay for β-adrenergic antagonist drugs

Robert B. Innis, David B. Bylund, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

A radioreceptor assay for β-adrenergic blocking drugs described here is based on the ability of the blood content of drugs to compete with the binding of 3H-dihydroalprenolol (3H-DHA) to β-adrenergic receptors in calf cerebellar membranes. Plasma protein greatly inhibits the binding of 3H-DHA to β-receptors by binding the 3H-DHA so it is unavailable to the β-receptors. As little as 0.01 ml of human plasma in a final volume of 1 ml reduces binding 25-45%. Assays conducted on plasma dialysates can be performed without such inhibition. The radioreceptor assay is simple to perform as 100 samples can be processed in a morning. It is sensitive, detecting low nanomolar concentrations of plasma propranolol, and it is specific. No drugs clinically employed other than β-blocking agents compete for β-receptor binding. The assay detects all pharmacologically active metabolites of β-blocking drugs as well as the parent drug.

Original languageEnglish (US)
Pages (from-to)2031-2037
Number of pages7
JournalLife Sciences
Volume23
Issue number20
DOIs
StatePublished - Nov 13 1978

Fingerprint

Radioligand Assay
Adrenergic Antagonists
Adrenergic Agents
Dihydroalprenolol
Assays
Pharmaceutical Preparations
Dialysis Solutions
Plasma (human)
Plasmas
Propranolol
Adrenergic Receptors
Blood Proteins
Metabolites
Blood
Membranes

ASJC Scopus subject areas

  • Pharmacology

Cite this

A simple, sensitive and specific radioreceptor assay for β-adrenergic antagonist drugs. / Innis, Robert B.; Bylund, David B.; Snyder, Solomon H.

In: Life Sciences, Vol. 23, No. 20, 13.11.1978, p. 2031-2037.

Research output: Contribution to journalArticle

Innis, Robert B. ; Bylund, David B. ; Snyder, Solomon H. / A simple, sensitive and specific radioreceptor assay for β-adrenergic antagonist drugs. In: Life Sciences. 1978 ; Vol. 23, No. 20. pp. 2031-2037.
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