Gardinier, Kevin M.; Gernert, Douglas L.; Porter, Warren J.; Reel, Jon K.; Ornstein, Paul L.; Spinazze, Patrick; Stevens, F. Craig; Hahn, Patric; Hollinshead, Sean P.; Mayhugh, Daniel; Schkeryantz, Jeff; Khilevich, Albert; De Frutos, Oscar; Gleason, Scott D.; Kato, Akihiko S.; Luffer-Atlas, Debra; Desai, Prashant V.; Swanson, Steven; Burris, Kevin D.; Ding, Chunjin; Heinz, Beverly A.; Need, Anne B.; Barth, Vanessa N.; Stephenson, Gregory A.; Diseroad, Benjamin A.; Woods, Tim A.; Yu, Hong; Bredt, David; Witkin, Jeffrey M. published an article about the compound: 3-(Chloromethyl)-1-methyl-1H-pyrazole( cas:84547-64-8,SMILESS:CN1N=C(CCl)C=C1 ).Electric Literature of C5H7ClN2. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:84547-64-8) through the article.
Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is one member of this family and is highly expressed within the hippocampus relative to the cerebellum. A selective TARP γ-8-dependent AMPA receptor antagonist (TDAA) is an innovative approach to modulate AMPA receptors in specific brain regions to potentially increase the therapeutic index relative to known non-TARP-dependent AMPA antagonists. We describe here, for the first time, the discovery of a noncompetitive AMPA receptor antagonist that is dependent on the presence of TARP γ-8. Three major iteration cycles were employed to improve upon potency, CYP1A2-dependent challenges, and in vivo clearance. An optimized mol., compound (-)-25 (LY3130481), was 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.
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Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics