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- Title
THE CGP7930 ANALOGUE 2,6-DI- TERT-BUTYL-4-(3-HYDROXY-2-SPIROPENTYLPROPYL)-PHENOL (BSPP) POTENTIATES BACLOFEN ACTION AT GABA<sub>B</sub> AUTORECEPTORS.
- Authors
Parker, David AS; Marino, Victor; Ong, Jennifer; Puspawati, Ni Made; Prager, Rolf H
- Abstract
1. The pharmacological actions of 2,6-di- tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP), a putative presynaptic GABAB receptor modulator, were examined in electrically stimulated rat neocortical brain slices preloaded with [3H]-GABA or [3H]-glutamic acid. 2. At 10 mmol/L, BSPP inhibited the release of [3H]-GABA in the presence of baclofen, but not that of [3H]-glutamic acid. This effect was sensitive to the GABAB receptor antagonist (+)-( S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch 50911). 3. Alone, BSPP had no effect on the release of [3H]-GABA or [3H]-glutamic acid. 4. It is concluded that BSPP selectively potentiates the action of baclofen at GABAB autoreceptors, but not heteroreceptors and may be a useful ligand to discriminate between presynaptic GABAB receptor subtypes.
- Publication
Clinical & Experimental Pharmacology & Physiology, 2008, Vol 35, Issue 9, p1113
- ISSN
0305-1870
- Publication type
Academic Journal
- DOI
10.1111/j.1440-1681.2008.04948.x