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Description: LY3130481 (also known as CERC-611) is a novel and potent alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist t that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) gamma-8, it selective inhibits AMPA/TARP gamma-8 with an IC50 of 65 nM. LY3130481 is fully protective against pentylenetetrazole-induced convulsions in rats without the motor impairment associated with non-TARP-dependent AMPA receptor antagonists. Compound (?)-25 could be utilized to provide proof of concept for antiepileptic efficacy with reduced motor side effects in patients.
References: J Med Chem. 2016 May 26; 59(10):4753-68.
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Delivery expected until 6/6/2024
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