Benzodiazepine receptors in human brain: characterization, subcellular localization and solubilization.
(1988) Progress in Neuro-Psychopharmacology & Biological Psychiatry — Vol. 12, n° 5, p. 773-782 (1988)
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- 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.
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Maloteaux, J.-M., Octave, J.-N., Vanisberg, M. A., Kollmann, P., Ackermans, A., & Laterre, C. (1988). Benzodiazepine receptors in human brain: characterization, subcellular localization and solubilization. Progress in Neuro-Psychopharmacology & Biological Psychiatry, 12(5), 773-782. https://doi.org/10.1016/0278-5846(88)90022-X (Original work published 1988)