Autoradiographic differentiation of multiple benzodiazepine receptors by detergent solubilization and pharmacologic specificity

We have used light microscopic autoradiography to localize differentially Type 1 and 2 benzodiazepine receptors using pharmacologic and detergent treatment techniques. The triazolopyridazine CL218872 has preferential affinity for Type 1 receptors from which it displaces [ 3H]flunitrazepam selectivel...

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Veröffentlicht in:Neuroscience letters 1983-08, Vol.39 (1), p.37-44
Hauptverfasser: Lo, Mathew M.S., Niehoff, Debra L., Kuhar, Michael J., Snyder, Solomon H.
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Sprache:eng
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Zusammenfassung:We have used light microscopic autoradiography to localize differentially Type 1 and 2 benzodiazepine receptors using pharmacologic and detergent treatment techniques. The triazolopyridazine CL218872 has preferential affinity for Type 1 receptors from which it displaces [ 3H]flunitrazepam selectively. In biochemical experiments [ 3H]flunitrazepam binding sites with pharmacologic properties of Type 2 receptors are preferentially solubilized from brain membranes by detergents. We have now treated rat brain slices either with CL218872 or 2% sodium cholate and evaluated the autoradiographic distribution of [ 3H]flunitrazepam-labeled receptors. Whether calculated from the drug or detergent treated preparations, the relative densities of apparent Type 1 and 2 receptors are the same. Thus differential sensitivity to detergent solubilization distinguishes the same two populations of receptors as Type 1 and 2 specific drugs.
ISSN:0304-3940
1872-7972
DOI:10.1016/0304-3940(83)90162-3