Maloteaux, Jean-Marie
[UCL]
Octave, Jean-Noël
[UCL]
Vanisberg, M. A.
Kollmann, P.
Ackermans, A.
Laterre, C.
1. Benzodiazepine receptors have been characterized in human brain mainly using [3H]-Ro 15-1788 and [3H]-flunitrazepam. Both ligands present a very high affinity for the receptor sites (Kd values of 0.56 and 1.53 nM respectively). 2. GABA enhanced the affinity of [3H]-flunitrazepam and [3H]-diazepam, but not that of [3H]-Ro 15-1788 and [3H]-methyl-beta-carboline 3-carboxylate for their specific binding sites as well in cerebral as in cerebellar human cortex. 3. Subcellular distribution of the benzodiazepine receptors revealed a main synaptosomal localization in human cerebral cortex, cerebellum and striatum. 4. Solubilized benzodiazepine receptors were obtained using 0.5% sodium deoxycholate and were characterized with [3H]-Ro 15-1788. The solubilized receptors are still coupled to GABA receptors since the [3H]-flunitrazepam specific binding was enhanced in the presence of micromolar concentrations of GABA.
Bibliographic reference |
Maloteaux, Jean-Marie ; Octave, Jean-Noël ; Vanisberg, M. A. ; Kollmann, P. ; Ackermans, A. ; et. al. Benzodiazepine receptors in human brain: characterization, subcellular localization and solubilization.. In: Progress in neuro-psychopharmacology & biological psychiatry, Vol. 12, no. 5, p. 773-82 (1988) |
Permanent URL |
http://hdl.handle.net/2078.1/11693 |