SIB 1757

SIB 1757

CAT N°: 35442
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From 65.00 55.25

SIB 1757 is an antagonist of metabotropic glutamate receptor 5a (mGluR5a).{64449} It selectively inhibits glutamate-induced calcium release and quisqualate-induced phosphoinositol accumulation in fibroblasts expressing human mGluR5a (IC50s = 0.37 and 3.1 µM, respectively) over mGluR1b-expressing fibroblasts (IC50s = >100 µM for both). SIB 1757 is also selective for mGluR5a over mGluR2, mGluR3, mGluR4a, mGluR6, mGluR7b, mGluR8 (IC50s = >100 µM for all), as well as AMPA, kainate, and NMDA receptors (IC50s = >30 µM for all). It inhibits phosphoinositol accumulation induced by the group I mGluR agonist (S)-3,5-DHPG (Item No. 14411) in isolated neonatal rat hippocampus and striatum (IC50s = 5.2 and 10.1 µM, respectively). Intrathecal administration of SIB 1757 (0.01 µg/animal) increases the paw withdrawal threshold in a rat model of neuropathic pain induced by spinal nerve ligation.{64450}

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