- 产品描述： E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation
- 靶点： mGluR
- 体外研究： E4CPG acts at rat cortical mGluR with the KB value of 0.367 mM
- 体内研究： E4CPG (3-30 nmol/site (i.t.), 1-10 μmol/paw (i.pl.), and 1-10 nmol/site (i.c.v.)) significantly inhibits the nociception induced by the Glutamate-injection (i.pl.; 30 μmol/paw), and the maximal inhibition values for the antinociceptive action of E4CPG in Glutamate-induced nociception are 48% (i.pl.), 49% (i.t.) and 40% (i.c.v.). E4CPG (35 nM/3.5 μL, i.c.v.) completely blocks long-term depression (LTD) induced by the group I mGluR agonist Dihydroxyphenylglycine (DHPG, 100 nM/5 μL, i.c.v.) in male Sprague-Dawley rats. Animal Model: Male Swiss mice (25-35 g) Dosage: 3-30 nmol/site (i.t.), 1-10 μmol/paw (i.pl.) and 1-10 nmol/ site (i.c.v.) Administration: Single injection Result: The maximal inhibition values for the antinociceptive action of E4CPG in glutamate-induced nociception were 48% (i.pl.), 49% (i.t.) and 40% (i.c.v.). Animal Model: Male Sprague-Dawley rats Dosage: 35 nM/3.5 μL Administration: Single injection, i.c.v. Result: Completely blocked LTD induced by the group I mGluR agonist dihydroxyphenylglycine (DHPG).
- 参考文献：
1. N Sekiyama, et al. Structure-activity relationships of new agonists and antagonists of different metabotropic glutamate receptorsubtypes. Br J Pharmacol, 1996 Apr, 117(7):1493-503. 2. Christian Patenaude, et al. GABAB receptor- and metabotropic glutamate receptor-dependent cooperative long-term potentiation of rat hippocampal GABAA synaptic transmission. J Physiol. 2003 Nov 15;553(Pt 1):155-67. 3. J S Bedingfield, et al. Structure-activity relationships for a series of phenylglycine derivatives acting at metabotropic glutamate receptors (mGluRs). Br J Pharmacol. 1995 Dec;116(8):3323-9. 4. Alessandra Beirith, et al. Mechanisms underlying the nociception and paw oedema caused by injection of glutamate into the mouse paw. Brain Res. 2002 Jan 11;924(2):219-28. 5. Jing Han, et al. Acute cannabinoids impair working memory through astroglial CB1 receptor modulation of hippocampal LTD. Cell. 2012 Mar 2;148(5):1039-50.
- 溶解性： Soluble in DMSO、H2O
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 4.48 ml 22.399 ml 44.798 ml 5 mM 0.896 ml 4.48 ml 8.96 ml 10 mM 0.448 ml 2.24 ml 4.48 ml 50 mM 0.09 ml 0.448 ml 0.896 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
