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Endogenous [ 3 H]flunitrazepam binding in human embryonic kidney cell line 293
- Source :
- European Journal of Pharmacology: Molecular Pharmacology; 19950115, Vol. 289 Issue: 0 p87-95, 9p
- Publication Year :
- 1995
-
Abstract
- Specific endogenous [ 3 H]flunitrazepam binding sites were identified and characterized in membranes from the human embryonic kidney (HEK) cell line 293. A large part of these binding sites exhibited an intermediate affinity for [ 3 H]flunitrazepam and a μM affinity for diazepam, clonazepam, 1-(2- chlorophenyl )-N- methyl -N-(1- methylpropyl )-3- isoquinolinecarboxamide (PK 11195) or 4′-chlorodiazepam (Ro 5-4864). These sites, thus, resembled neither γ-aminobutyric acid A (GABA A ) receptor associated nor 'peripheral' benzodiazepine binding sites. A small part of the binding sites labeled by [ 3 H]flunitrazepam seemed to belong to 'peripheral' benzodiazepine binding sites exhibiting a nM affinity for PK 11195, and another small part of the binding sites seemed to exhibit a high affinity for flunitrazepam and PK 11195. Although small amounts of mRNA for α 1 -, β 3 - and γ 2 - subunits of GABA A receptors could be identified in HEK 293 cells, neither the actual expression of GABA A receptors in these cells nor a coassembly of endogenous subunits with transfected GABA A receptor subunits could be demonstrated by binding studies.
Details
- Language :
- English
- ISSN :
- 09224106
- Volume :
- 289
- Issue :
- 0
- Database :
- Supplemental Index
- Journal :
- European Journal of Pharmacology: Molecular Pharmacology
- Publication Type :
- Periodical
- Accession number :
- ejs4005095
- Full Text :
- https://doi.org/10.1016/0922-4106(95)90172-8