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Benzodiazepine Receptor Modulation of [35S]TBPS Binding to the Chloride Channel. Noncompetitive Inhibition of Classical Benzodiazepines and Competitive Inhibition of the Partial Agonist, CGS 9895, by CGS 8216

Benzodiazepine Receptor Modulation of [35S]TBPS Binding to the Chloride Channel. Noncompetitive Inhibition of Classical Benzodiazepines and Competitive Inhibition of the Partial Agonist, CGS 9895, by CGS 8216

P Loo, A Braunwalder, P L Wood

Neuropharmacology. 1987 Jul;26(7A):775-8.

PMID: 2442653

Abstract:

Benzodiazepine receptor ligands are known to modulate the binding of [35S]TBPS to the chloride channel via an allosteric action. In the cases of diazepam, zopiclone and CGS 9895, the enhanced binding of [35S]TBPS induced by these benzodiazepine agonists was antagonized by CGS 8216. This antagonism was characterized both by a shift to the right and a decrease in the maximal stimulation, for the dose-response curves of diazepam and zopiclone. In the case of CGS 9895, the maximal response was not decreased. These data indicate that CGS 8216 is a noncompetitive antagonist of classical benzodiazepine receptor agonists but is a competitive inhibitor of the partial agonist, CGS 9895.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP77779501	CGS 9895		77779-50-1	Price

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