Evaluation of a radioreceptor assay for beta-adrenoceptor antagonists in plasma.

Abstract:

:A radioreceptor assay (RRA) recently developed in this laboratory for beta-adrenoceptor antagonists in plasma was evaluated in normal volunteers and compared with a radioimmunoassay (RIA) for propranolol. The RRA depends upon the ability of beta-adrenoceptor antagonists to complete with a radiolabelled ligand for beta-adrenoceptor binding sites on lung membranes. Unlike other assays, it measures biologically active drugs including active metabolites of the parent compound. In volunteers given a single oral dose of (+/-)-propranolol, considerable differences between the two assay methods were demonstrated. In other experiments this difference was shown to relate to the RIA's sensitivity to the inactive (+)-isomer of propranolol and possibly to inactive metabolites. The facility of the RRA in measuring plasma levels of several other non-selective beta-adrenoceptor antagonists was also demonstrated. By employing (-)-propranolol as the standard in the RRA, all of these drugs can be directly compared with a single and relatively simple assay technique.

journal_name

Eur J Clin Pharmacol

authors

Barnett DB,Batta M,Davies B,Nahorski SR

doi

10.1007/BF00558447

subject

Has Abstract

pub_date

1980-05-01 00:00:00

pages

349-54

issue

5

eissn

0031-6970

issn

1432-1041

journal_volume

17

pub_type

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