YM-230888 is a selective allosteric antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting a binding affinity (Ki) of 13 nM. It effectively inhibits the production of inositol phosphates in rat cerebellar granule cells, with an IC50 of 13 nM. Research indicates that YM-230888 possesses significant antinociceptive effects in models of hyperalgesia induced by Streptozotocin, as well as in complete Freund's adjuvant-induced arthritis pain models, highlighting its potential utility in pain management studies.
YM-230888 is a selective allosteric antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting a binding affinity (Ki) of 13 nM. It effectively inhibits the production of inositol phosphates in rat cerebellar granule cells, with an IC50 of 13 nM. Research indicates that YM-230888 possesses significant antinociceptive effects in models of hyperalgesia induced by Streptozotocin, as well as in complete Freund's adjuvant-induced arthritis pain models, highlighting its potential utility in pain management studies.
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