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Description: JNJ-55511118 is a novel, high affinity and selective negative modulator of AMPA receptors containing TARP-gamma8 (Ki = 26 nM). JNJ-55511118 had excellent pharmacokinetic properties and achieved high receptor occupancy following orally bioavailable administration. JNJ-55511118 showed strong, dose-dependent inhibition of neurotransmission within the hippocampus, and a strong anticonvulsant effect.
References: Maher MP, Wu N, Ravula S, Ameriks MK, Savall BM, Liu C, Lord B, Wyatt RM, Matta JA, Dugovic C, Yun S, Ver Donck L, Steckler T, Wickenden AD, Carruthers NI, Lovenberg TW. Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-gamma8. J Pharmacol Exp Ther. 2016 May; 357(2):394-414.
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