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XAP044 is an antagonist of the metabotropic glutamate (mGlu) receptor 7 (mGluR7), inhibiting lateral amygdala long term potentiation in brain slices from wild-type mice with an IC50 value of 88 nM.1 This effect is absent in mGluR7-deficient mice. XAP044 demonstrates good brain penetrance, producing wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral tests.1
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1. Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-