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CGP52432

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Chemical Structure| 139667-74-6 同义名 : -
CAS号 : 139667-74-6
货号 : A885418
分子式 : C15H24Cl2NO4P
纯度 : 99%+
分子量 : 384.235
MDL号 : MFCD09878290
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(10.41 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 4 mg/mL(10.41 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 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[1]. CGP52432 exhibited intrinsic activity only in the hippocampus; in spinal cord, it behaved exclusively as a silent orthosteric antagonist by blocking the release inhibition brought about by (-)-baclofen[2]. CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze[3]. Treatment with the GABAB receptor antagonist CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolished the suppressive effects of 50 μmol/kg, i.v., GABA on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, leading to elimination of the renoprotective effects of GABA[4]. CGP52432 (a GABAB receptor antagonist) at intravenous dosages of 0.1-1 mg/kg completely removed the TNS (tibial nerve stimulation) inhibition in female cats but had no effect in male cats. CGP52432 administered intravenously also had no effect on control bladder capacity or the pudendal inhibition of bladder overactivity[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.03mL

5.21mL

2.60mL
参考文献

[1]Lanza M, Fassio A, Gemignani A, Bonanno G, Raiteri M. 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]Romei C, Luccini E, Raiteri M, Raiteri L. The GABA B receptor antagonists CGP35348 and CGP52432 inhibit glycine exocytosis: study with GABA B1- and GABA B2-deficient mice. Pharmacol Res. 2010 Jun;61(6):547-52

[3]Sweeney FF, O'Leary OF, Cryan JF. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10

[4]Kobuchi S, Tanaka R, Shintani T, Suzuki R, Tsutsui H, Ohkita M, Matsumura Y, Ayajiki K. 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

[5]Fuller TW, Jiang X, Bansal U, Lamm V, Shen B, Wang J, Roppolo JR, de Groat WC, Tai C. Sex difference in the contribution of GABAB receptors to tibial neuromodulation of bladder overactivity in cats. Am J Physiol Regul Integr Comp Physiol. 2017 Mar 1;312(3):R292-R300