Abstract
GTP decreases the specific binding of [3H]flunitrazepam to cerebral cortical membrane sites. Scatchard analysis data show that GTP does not alter the maximum binding sites (Bmax), but increases the dissociation constant (KD) for [3H]flunitrazepam. GTP also inhibits the specific binding of the benzodiazepine antagonist [3H]CGS-8216. The specific binding of [3H]CGS-8216 displaceable by clonazepam is inhibited to a greater extent by GTP than that displaceable by the benzodiazepine antagonists, CGS-8216 or beta-CCE.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzodiazepines / antagonists & inhibitors
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Binding, Competitive / drug effects
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Brain / metabolism*
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Cattle
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Cell Membrane / metabolism
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Flunitrazepam / metabolism
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Guanosine Triphosphate / pharmacology*
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In Vitro Techniques
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Pyrazoles / metabolism
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Receptors, Drug / drug effects*
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Receptors, Drug / metabolism
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Receptors, GABA-A
Substances
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Pyrazoles
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Receptors, Drug
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Receptors, GABA-A
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Benzodiazepines
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Flunitrazepam
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2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one
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Guanosine Triphosphate