货号 | 1248/50 |
别名 | (2S)-3-[[(1S)-1-(3,4-Dichlorophenyl |
供应商 | Tocris |
生物活性 | Potent, selective GABAB receptor antagonist (IC50 = 5 nM) that prevents agonist binding (pKi = 8.35) and inhibits GABA and glutamate release (pEC50 values are 8.08 and 7.85 respectively). Inhibits GABAB responses to baclofen (IC50 = 130 nM in an isoproterenol assay) and potentiates the hypoglycemic response to glucose in vitro. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 438.71 |
分子式 | C18H22Cl2NO3P.HCl |
可溶性/溶解性 | Soluble to 100 mM in DMSO with gentle warming |
CAS号 | 149184-22-5 |
参考文献 | Salah and Perkins (2008) Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology 55 47. PMID: 18538357. Zhanget al (2007) Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. J.Physiol. 578 735. PMID: 17124268. Deisz (1999) The GABAB antagonist CGP 55845A reduces presynaptic GABA1 actions in neurons of the rat in vitro. Neuroscience 93 1241. PMID: 10501448. Cunninghan and Enna (1996) Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain. Brain Res. 720 220. PMID: 8782915. Froestlet al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8127. Waldmeieret al (1994) GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. Br.J.Pharmacol. 113 1515. PMID: 7889310. |