Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.3.1.107 (
DAT
)
1,471
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Herein, we report the discovery of the first selective and CNS penetrant mGlu
7
PAM
(VU6027459) derived from a "molecular switch" within a selective mGlu
7
NAM chemotype. VU6027459 displayed CNS penetration in both mice (K
p
= 2.74) and rats (K
p
= 4.78), it was orally bioavailable in rats (%F = 69.5), and undesired activity at
DAT
was ablated.
...
PMID:Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu
7
Positive Allosteric Modulator Tool Compound. 3294 46
