1.
ACS Med Chem Lett
; 11(9): 1773-1779, 2020 Sep 10.
Article
in English
| MEDLINE
| ID: mdl-32944146
ABSTRACT
Herein, we report the discovery of the first selective and CNS penetrant mGlu7 PAM (VU6027459) derived from a "molecular switch" within a selective mGlu7 NAM chemotype. VU6027459 displayed CNS penetration in both mice (Kp = 2.74) and rats (Kp= 4.78), it was orally bioavailable in rats (%F = 69.5), and undesired activity at DAT was ablated.
