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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(B) autoreceptors|
|Citation:||Clinical and Experimental Pharmacology and Physiology, 2008; 35(9):1113-1115|
|Publisher:||Blackwell Publishing Asia|
|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|
|Appears in Collections:||Medicine publications|
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