| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
SR 95531 hydrobromide (Gabazine) to be a selective antagonist at the GABA binding sites on GABAA receptors.
Animal models | Male ICR mice |
Preparation Method | Effects of 5-aminovaleric acid (5-AVA) and SR 95531 injected intrathecally (i.t.) on inhibition of the tail-flick response induced by DSC administered i.t. Saline (5 µl), 5-AVA (from 1 to 20 µg) or SR 95531 (from 0.1 to 2 ng) was pretreated i.t. 10 min before i.t. administration of DSC (30 µg) or vehicle. |
Dosage form | injected intrathecally, 0.1 to 2 ng |
Applications | SR 95531 attenuated i.t. administered DSC-induced inhibition of the tail-flick response in a dose-dependent manner. |
| 产品描述 | SR 95531 hydrobromide (Gabazine) to be a selective antagonist at the GABA binding sites on GABAA receptors[1]. SR 95531 hydrobromide partially inhibited direct activation of the receptor by the barbiturate pentobarbital and by the steroid alphaxolone, possibly by acting as an allosteric inhibitor of GABAA receptor channel opening[2]. SR 95531 hydrobromide had antagonist potency response against to the binding of GABA and recombination α1β2γ2S GABAA receptors, with the IC50 of 349 nM[1]. The competitive antagonist SR 95531 hydrobromide showed similar potency on both cell types with IC50's of 196 nM and 224 nM on α4β3γ2 receptors and α4β3δ receptors respectively[3]. In αTC1-9 cells, GABA (10 μmol/l) significantly suppressed glucagon secretion to ~50% of control levels, whereas in the presence of SR 95531 hydrobromide (10 μmol/l), exogenous GABA exerted no significant effect on glucagon secretion[4]. SR 95531 hydrobromide administered i.t. effectively attenuated antinociception induced by i.t. administered Dipsacus saponin C (DSC)[5]. References: |
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