Document Report Card
Basic Information
ID: ALA4665820
Journal: ACS Med Chem Lett
Title: Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu Positive Allosteric Modulator Tool Compound.
Authors: Reed CW,Kalbfleisch JJ,Wong MJ,Washecheck JP,Hunter A,Rodriguez AL,Blobaum AL,Conn PJ,Niswender CM,Lindsley CW
Abstract: Herein, we report the discovery of the first selective and CNS penetrant mGlu PAM (VU6027459) derived from a "molecular switch" within a selective mGlu NAM chemotype. VU6027459 displayed CNS penetration in both mice (K = 2.74) and rats (K= 4.78), it was orally bioavailable in rats (%F = 69.5), and undesired activity at DAT was ablated.
CiteXplore: 32944146