Possible Interaction: Gamma-Aminobutyric Acid and Gaba Antagonists

“The inhibitory effects of gamma-amino butyric acid (GABA) were disinhibited by the GABABR antagonist CGP-35348 or GABABR knockdown.”

“The open probability (P(o)) of both K(Na) and K(Ca) channels was found to be increased by bath application of GABA , and this increase in Po was antagonized by coapplication of the GABAB antagonist CGP54626, suggesting that GABA(B)-like receptors mediate these actions.”

“Furthermore, the GABAB receptor antagonist , SCH-50911, prevents GABA or synaptically induced depression.”

“ GABA significantly increased melatonin levels in a dose‐dependent manner, its effect being reversed by a GABAA receptor antagonist , bicuculline, but not by saclofen, a GABAB antagonist.”

“The gastrin and somatostatin responses to 10–4 M GABA were completely inhibited by the GABAA antagonist bicuculline (10–5 M) and the cholinergic blocker atropine (10–7 M), whereas the GABAB antagonist CGP 35348 (5 × 10–5 M) was ineffective.”

“… GABA‐A antagonist bicucilline (50 μM) was ineffective when infused locally …, but prolonged the increase in neuronal GABA release after nigral stimulation; the GABA levels were increased during two 3‐min samples to ∼165%, … role for GABA‐A receptors in regulating the release of GABA from nigrothalamic GABAergic neurons.”

“The effect of GABA was concentration-dependent (1-1000 microM) and was blocked by a GABAA receptor antagonist , bicuculline (100 microM), or a GABAA chloride channel blocker, picrotoxin (100 microM), but not by a GABAB receptor antagonist, 2-hydroxysaclofen (100 microM).”

“The effect was marginally significant at 1 microM and … at 20 microM. The action of 20 microM GABA was mimicked by the GABAB-receptor agonist, muscimol, but not … the GABAA-receptor agonist, baclofen, and completely blocked by the GABAA-receptor antagonists , bicuculline and picrotoxin, which lacked effect per se.”

“Lightening of skin color with dopamine was inhibited by a D2 receptor antagonist (sulpiride), and the effect of GABA was blocked by both sulpiride and a GABAA receptor antagonist (bicuculline).”

“The effect of GABA was counteracted by the GABAB receptor antagonist CGP 35348 [P-(3-aminopropyl)-P-diethoxymethylphosphinic acid] but was not influenced by the GABAA receptor antagonist SR 95531 [2-(3-carboxypropyl)-3-amino-6-paramethoxyphenylpyridazinium bromide].”