1040724-12-6Relevant articles and documents
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)
Reed, Carson W.,Yohn, Samantha E.,Washecheck, Jordan P.,Roenfanz, Hanna F.,Quitalig, Marc C.,Luscombe, Vincent B.,Jenkins, Matthew T.,Rodriguez, Alice L.,Engers, Darren W.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Lindsley, Craig W.
supporting information, p. 1690 - 1695 (2019/02/24)
Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu7) negative allosteric modulator (NAM) that achieves exposure in cerebral spinal fluid (CSF) 2.5× above the in vitro IC50 at minimum effective doses (MEDs) of 3 mg/kg in preclinical anxiety models.
NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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Page/Page column 56-57, (2008/12/07)
The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.