1982
DOI: 10.1111/j.1365-2125.1982.tb01422.x
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A radioreceptor assay to study the affinity of benzodiazepines and their receptor binding activity in human plasma including their active metabolites.

Abstract: 1 A radioreceptor assay has been established to measure the receptor affinities of numerous benzodiazepines in clinical use. 2 The time course of receptor binding activity was studied by this method in the plasma of eight healthy subjects randomly treated with 1 mg lormetazepam (Noctamid, 2 mg flunitrazepam (Rohypnol, and 10 mg diazepam (Valium, and placebo on a cross-over basis. Blood samples were collected up to 154 h after treatment. 3 Receptor affinities of numerous benzodiazepines on vitro show good corre… Show more

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Cited by 32 publications
(9 citation statements)
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“…in comparison with placebo. These results agree with the high receptor affinity (Dorow et al, 1982) of lormetazepam in vitro. The increase in heart rate reached a significant level in the first and second hours p.a.…”
Section: Discussionsupporting
confidence: 90%
“…in comparison with placebo. These results agree with the high receptor affinity (Dorow et al, 1982) of lormetazepam in vitro. The increase in heart rate reached a significant level in the first and second hours p.a.…”
Section: Discussionsupporting
confidence: 90%
“…Plasma levels of ligands binding to the BZ receptor, i.e. BZ (FNZ and LMZ) (data not shown) and Ro 15-1788 (Klotz et al 1984), were monitored on both experimental days with a BZ radioreceptor assay (Dorow et al 1982) and/or a HPLC assay (Timm and Zell 1983). Measurement of BZ binding equivalents in plasma 24 h after treatment showed still significant values for both BZ-treated groups: FNZ binding equivalents (ng/ml) -FNZ group 4.87 4-1.8; LMZ group 3.02+_ 1.38.…”
Section: Resultsmentioning
confidence: 99%
“…Coefficients of inter-or intra-assay variations were 7% and 6%, respectively. Concentrations of benzodiazepine binding equivalents in plasma were measured with a radioreceptor assay (Dorow et al 1982). For statistical evaluation the Wilcoxon matched paired test and Mann-Whitney U-test were employed.…”
Section: Methodsmentioning
confidence: 99%
“…These specific affinities are justified by the choice of the competitor ligand and the kind of receptor tissue material. Indeed, flunitrazepam which is a fluorine nitrazepam derivative was selected because of its high affinity for benzodiazepine receptors [39]. In the same way, spiperone and DAMGO have respectively high affinity for dopaminergic and µ receptors.…”
Section: Discussionmentioning
confidence: 99%