1027176-31-3Relevant academic research and scientific papers
Phenyl-tetrazolyl acetophenones: Discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor
Pinkerton, Anthony B.,Vernier, Jean-Michel,Schaffhauser, Hervé,Rowe, Blake A.,Campbell, Una C.,Rodriguez, Dana E.,Lorrain, Daniel S.,Baccei, Christopher S.,Daggett, Lorrie P.,Bristow, Linda J.
, p. 4595 - 4599 (2004)
Herein we disclose the discovery of a new class of positive allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2), phenyl-tetrazolyl acetophenones, e.g. 1-(2-hydroxy-3-propyl-4-{4-[4-(2H-tetrazol-5-yl)phenoxy] butoxy}phenyl) ethanone (4
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones
Pinkerton, Anthony B.,Cube, Rowena V.,Hutchinson, John H.,Rowe, Blake A.,Schaffhauser, Hervé,Zhao, Xiumin,Daggett, Lorrie P.,Vernier, Jean-Michel
, p. 5329 - 5332 (2007/10/03)
We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC50 = 93 nM, 128% potentiation). We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC50 = 93 nM, 128% potentiation).
