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Discovery of VU6005649, a CNS Penetrant mGlu 7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5- a ]pyrimidines.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2017 Sep 01; Vol. 8 (10), pp. 1110-1115. Date of Electronic Publication: 2017 Sep 01 (Print Publication: 2017). - Publication Year :
- 2017
-
Abstract
- Herein, we report the structure-activity relationships within a series of mGlu <subscript>7</subscript> PAMs based on a pyrazolo[1,5- a ]pyrimidine core with excellent CNS penetration ( K <subscript>p</subscript> s > 1 and K <subscript>p,uu</subscript> s > 1). Analogues in this series proved to display a range of Group III mGlu receptor selectivity, but VU6005649 emerged as the first dual mGlu <subscript>7/8</subscript> PAM, filling a void in the Group III mGlu receptor PAM toolbox and demonstrating in vivo efficacy in a mouse contextual fear conditioning model.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 8
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 29057060
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.7b00317