Enhancement of the binding of 3H-diazepam to rat brain membranes in vitro by SQ 20009, A novel anxiolytic, gamma-aminobutyric acid (GABA) and muscimol. |
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Authors: | M Williams E A Risley |
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Affiliation: | Neuropsychopharmacology Section Merck Institute for Therapeutic Research West Point, Pennsylvania 19486, USA |
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Abstract: | SQ 20009, a compound with anxiolytic-like activity, was found to cause an enhancement of the binding of 3H-diazepam to rat brain membranes in a concentration-dependent manner with inhibition of binding occuring at 10?4 M. Both GABA and the GABA agonist, muscimol, were also found to enhance 3H-diazepam binding while the GABA antagonist (+)-bicuculline decreased binding. The effects of SQ 20009, the GABA agonists and (+)-bicuculline were reflected as a change in the affinity rather than number of binding sites. The effects of SQ 20009 and GABA and muscimol are discussed in terms of an interaction with an endogenous diazepam-like factor. |
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