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https://hdl.handle.net/2440/53528
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Type: | Journal article |
Title: | The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors |
Author: | Parker, D. Marino, V. Ong, J. Puspawati, N. Prager, R. |
Citation: | Clinical and Experimental Pharmacology and Physiology, 2008; 35(9):1113-1115 |
Publisher: | Blackwell Publishing Asia |
Issue Date: | 2008 |
ISSN: | 0305-1870 1440-1681 |
Statement of Responsibility: | David AS Parker, Victor Marino, Jennifer Ong, Ni Made Puspawati and Rolf H Prager |
Abstract: | The pharmacological actions of 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP), a putative presynaptic GABA(B) receptor modulator, were examined in electrically stimulated rat neocortical brain slices preloaded with [3H]-GABA or [3H]-glutamic acid. 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 GABA(B) receptor antagonist (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch 50911). Alone, BSPP had no effect on the release of [3H]-GABA or [3H]-glutamic acid. It is concluded that BSPP selectively potentiates the action of baclofen at GABA(B) autoreceptors, but not heteroreceptors and may be a useful ligand to discriminate between presynaptic GABA(B) receptor subtypes. |
Keywords: | Neocortex Animals Rats Rats, Sprague-Dawley Tritium gamma-Aminobutyric Acid Baclofen Phenols Morpholines Spiro Compounds Glutamic Acid Receptors, GABA-B Organ Culture Techniques Drug Evaluation, Preclinical Drug Synergism Male GABA-B Receptor Antagonists |
Description: | The definitive version may be found at www.wiley.com |
DOI: | 10.1111/j.1440-1681.2008.04948.x |
Published version: | http://dx.doi.org/10.1111/j.1440-1681.2008.04948.x |
Appears in Collections: | Aurora harvest Medicine publications |
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