Nelson, Derek W. published the artcileStructure-Activity Relationship Studies on a Series of Novel, Substituted 1-Benzyl-5-phenyltetrazole P2X7 Antagonists, Name: 2,3-Dimethoxybenzonitrile, the main research area is enzylphenyltetrazole derivative SAR preparation P2X7 receptor antagonist.
1-Benzyl-5-aryltetrazoles were discovered to be novel antagonists for the P2X7 receptor. Structure-activity relationship (SAR) studies were conducted around both the benzyl and Ph moieties. In addition, the importance of the regiochem. substitution on the tetrazole was examined Compounds were evaluated for activity to inhibit calcium flux in both human and rat recombinant P2X7 cell lines using fluorometric imaging plate reader technol. Analogs were also assayed for their ability to inhibit IL-1β release and to inhibit P2X7-mediated pore formation in human THP-1 cells. Compound 15d was advanced to efficacy studies in a model of neuropathic pain where significant reversal of mech. allodynia was observed at doses that did not affect motor coordination.
Journal of Medicinal Chemistry published new progress about Allodynia. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Name: 2,3-Dimethoxybenzonitrile.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts