RG-7090

RG-7090

CAT N°: 36806
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From 128.00 108.80

RG-7090 is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5).{66139} It binds to mGluR5 (Ki = 35.6 nM) and is selective for mGluR5 over a panel of 116 additional receptors at 10 µM. RG-7090 inhibits quisqualate-induced calcium mobilization and inositol phosphate accumulation in HEK293 cells expressing human mGluR5 (IC50s = 7 and 5.9 nM, respectively). In vivo, RG-7090 (10 and 30 mg/kg) reduces immobility time in the forced swim test in rats. It increases drinking time in the Vogel conflict drinking test and reduces stress-induced hyperthermia, indicating anxiolytic-like activity, in rats. RG-7090 (0.1-10 mg/kg, s.c.) inhibits surgical sciatic nerve constriction-induced cold allodynia in rats. It also increases the threshold of bladder filling volume to trigger the micturition reflex in anesthetized rats.

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