693288-96-9Relevant academic research and scientific papers
Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA
Zhao, Zhijian,Wisnoski, David D.,O'Brien, Julie A.,Lemaire, Wei,Williams Jr., David L.,Jacobson, Marlene A.,Wittman, Marion,Ha, Sookhee N.,Schaffhauser, Herve,Sur, Cyrille,Pettibone, Doug J.,Duggan, Mark E.,Conn, P. Jeffrey,Hartman, George D.,Lindsley, Craig W.
, p. 1386 - 1391 (2007/10/03)
This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to
A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain
O'Brien, Julie A.,Lemaire, Wei,Wittmann, Marion,Jacobson, Marlene A.,Ha, Sookhee N.,Wisnoski, David D.,Lindsley, Craig W.,Schaffhauser, Herve J.,Rowe, Blake,Sur, Cyrille,Duggan, Mark E.,Pettibone, Douglas J.,Conn, P. Jeffrey,Williams Jr., David L.
, p. 568 - 577 (2007/10/03)
We found that N-{4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl} -2-hydroxybenzamide (CPPHA), is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). CPPHA alone had no agonist
