Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 84547-64-8, is researched, SMILESS is CN1N=C(CCl)C=C1, Molecular C5H7ClN2Journal, Article, Journal of Medicinal Chemistry called Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8, Author is 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., the main research direction is LY3130481 preparation AMPA receptor antagonist TARP gamma8 anticonvulsant epilepsy.Electric Literature of C5H7ClN2.
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.
As far as I know, this compound(84547-64-8)Electric Literature of C5H7ClN2 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.
Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics