ISSN:
1432-1041
Keywords:
propranolol
;
radioreceptor assay
;
beta-adrenoceptor antagonists
;
lung membranes
;
plasma level
;
healthy volunteers
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Summary 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 compete 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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00558447
Permalink
