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• W2891551577 abstract "This work describes the discovery and characterization of novel 6-(1 H-pyrazolo[4,3- b]pyridin-3-yl)amino-benzo[ d]isothiazole-3-carboxamides as mGlu4 PAMs. This scaffold provides improved metabolic clearance and CYP1A2 profiles compared to previously discovered mGlu4 PAMs. From this work, 27o (VU6001376) was identified as a potent (EC50 = 50.1 nM, 50.5% GluMax) and selective mGlu4 PAM with an excellent rat DMPK profile ( in vivo rat CLp = 3.1 mL/min/kg, t1/2 = 445 min, CYP1A2 IC50 > 30 μM). Compound 27o was also active in reversing haloperidol induced catalepsy in a rodent preclinical model of Parkinson's disease." @default.
• W2891551577 created "2018-09-27" @default.
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• W2891551577 date "2018-09-24" @default.
• W2891551577 modified "2023-09-24" @default.
• W2891551577 title "Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6-((1<i>H</i>-Pyrazolo[4,3-<i>b</i>]pyridin-3-yl)amino)-benzo[<i>d</i>]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu₄)" @default.
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• W2891551577 doi "https://doi.org/10.1021/acs.jmedchem.8b00994" @default.
• W2891551577 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30247901" @default.
• W2891551577 hasPublicationYear "2018" @default.
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