JNJ-46356479 is a Selective and orally Bioavailable mGlu2 receptor Positive Allosteric Modulator (PAM). JNJ-46356479 showed mGlu2 PAM EC50=78 nM; mGlu2 PAM Emax (%) = 256. JNJ-46356479 is in vivo active, sw-EEG at 3mg/kg, p.o. JNJ-46356479 represents a more balanced profile that offers a significant improvement on the druglike attributes compared to previously reported leads. References: Cid JM, Tresadern G, Vega JA, de Lucas AI, Del Cerro A, Matesanz E, Linares ML, García A, Iturrino L, Pérez-Benito L, Macdonald GJ, Oehlrich D, Lavreysen H, Peeters L, Ceusters M, Ahnaou A, Drinkenburg W, Mackie C, Somers M, Trabanco AA. Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 receptor Positive Allosteric Modulator (PAM). J Med Chem. 2016 Aug 31. [Epub ahead of print] PubMed PMID: 27579727.

纯度：≥98%

CAS：1254979-66-2