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THE CGP7930 ANALOGUE 2,6‐DI‐ TERT ‐BUTYL‐4‐(3‐HYDROXY‐2‐SPIROPENTYLPROPYL)‐PHENOL (BSPP) POTENTIATES BACLOFEN ACTION AT GABA B AUTORECEPTORS
Author(s) -
Parker David AS,
Marino Victor,
Ong Jennifer,
Puspawati Ni Made,
Prager Rolf H
Publication year - 2008
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.2008.04948.x
Subject(s) - baclofen , autoreceptor , gabab receptor , chemistry , glutamic acid , receptor , antagonist , agonist , aminobutyric acid , pharmacology , stereochemistry , amino acid , biochemistry , biology
SUMMARY1 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 [ 3 H]‐GABA or [ 3 H]‐glutamic acid. 2 At 10 mmol/L, BSPP inhibited the release of [ 3 H]‐GABA in the presence of baclofen, but not that of [ 3 H]‐glutamic acid. This effect was sensitive to the GABA B receptor antagonist (+)‐( S )‐5,5‐dimethylmorpholinyl‐2‐acetic acid (Sch 50911). 3 Alone, BSPP had no effect on the release of [ 3 H]‐GABA or [ 3 H]‐glutamic acid. 4 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.