| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | E4CPG acts at rat cortical mGluR with the KB value of 0.367 mM[3]. | ||||||||||||
| In Vivo | 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.) [4]. 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[5]. Animal Model: | ||||||||||||
| Name | E4CPG | ||||||||||||
| CAS | 170846-89-6 | ||||||||||||
| Formula | C11H13NO4 | ||||||||||||
| Molar Mass | 223.23 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |