Discovery of N-Aryl Piperazines as Selective mGluR5 Potentiators with Improved In Vivo Utility was written by Zhou, Ya;Manka, Jason T.;Rodriguez, Alice L.;Weaver, C. David;Days, Emily L.;Vinson, Paige N.;Jadhav, Satyawan;Hermann, Elizabeth J.;Jones, Carrie K.;Conn, P. Jeffrey;Lindsley, Craig W.;Stauffer, Shaun R.. And the article was included in ACS Medicinal Chemistry Letters in 2010.SDS of cas: 175205-82-0 This article mentions the following:
This letter describes the discovery, structure-activity relation, and in vitro and in vivo pharmacol. profile of a novel non-MPEP-derived mGluR5 pos. allosteric modulator (PAM) based upon an N-aryl piperazine chemotype. This mGluR5 chemotype exhibits the ability to act as either a noncompetitive antagonist/neg. allosteric modulator or a potentiator of the glutamate response, depending on the identity of the amide substituent, i.e., a “mol. switch”. A rapidly optimized PAM, 10e (VU0364289), was shown to be potent and specific for the rat mGluR5 receptor and subsequently demonstrated to be efficacious in a clin. relevant rodent model predictive of antipsychotic activity, thus providing the first example of a centrally active mGluR5 PAM optimized from an HTS-derived mGluR5 noncompetitive antagonist. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0SDS of cas: 175205-82-0).
2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.SDS of cas: 175205-82-0