S87840 |
CGP 52432 |
源叶(MedMol) | 98% |
- 产品描述: CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
- 靶点: IC50: 85 nM (GABAB receptor);GABAReceptor
- 体外研究:
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM, 35- and 100-fold lower than at the receptors regulating somatostatin and glutamate overflow, respectively
- 体内研究:
CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze. CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolishes the suppressive effects of GABA ( 50 μmol/kg, i.v.) on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, causeing elimination of the renoprotective effects of GABA in rats
- 参考文献:
1. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5. 2. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10. 3. Kobuchi S, et al. Mechanisms underlying the renoprotective effect of GABA against ischaemia/reperfusion-induced renal injury in rats. Clin Exp Pharmacol Physiol. 2015 Mar;42(3):278-86.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: 2-8°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.603 ml 13.013 ml 26.025 ml 5 mM 0.521 ml 2.603 ml 5.205 ml 10 mM 0.26 ml 1.301 ml 2.603 ml 50 mM 0.052 ml 0.26 ml 0.521 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)