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E4CPG is an antagonist of metabotropic glutamate receptor 1 (mGluR1) and mGluR2.1 It is selective for mGluR1 and mGluR2 over mGluR6 at 1 mM. E4CPG (1 mM) inhibits L-glutamate-induced increases in inositol phosphate (InsP) levels in CHO cells expressing mGluR1 and prevents forskolin-induced decreases in cAMP levels in CHO cells expressing mGluR2. In vivo, intraplantar administration of E4CPG (1-10 nmol/paw) reduces glutamate-induced paw licking in a mouse model of nociceptive pain.2
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1. Structure-
2. Mechanisms underlying the nociception and paw oedema caused by injection of glutamate into the mouse paw. Brain Res. 924(2), 219-228 (2002).