Flunitrazepam binding sites in rat diaphragm. Receptors for direct neuromuscular effects of benzodiazepines?
- 1 July 1982
- journal article
- Published by Canadian Science Publishing in Canadian Journal of Physiology and Pharmacology
- Vol. 60 (7) , 1003-1005
- https://doi.org/10.1139/y82-142
Abstract
The evidence for direct muscle relaxant effects of benzodiazepines is controversial. We now show that a crude membrane preparation of rat diaphragm possesses binding sites for [3H]flunitrazepam (FNZ). Scatchard analysis gave a binding site density of 1689 ± 143 fmol/mg protein (Kd = 25.6 ± 2.6 nM). These sites are of the "peripheral" type since clonazepam fails to displace [3H]FNZ as effectively as R05-4864 (IC50 values: 7.5 × 10 6 M and 8 × 10−9 M, respectively). Diazepam is almost as effective as R05-4864 and potently displaces [3H]FNZ binding (IC50 = 3 × 10−8 M). We propose that the previously described effects of diazepam on rat diaphragm are mediated through high-affinity binding sites.Keywords
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