Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.

Sharma S, Rodriguez AL, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2008 18 (14): 4098-101

PMID: 18550372 · PMCID: PMC2533619 · DOI:10.1016/j.bmcl.2008.05.091

MeSH Terms (16)

Allosteric Regulation Allosteric Site Animals Binding, Competitive Chemistry, Pharmaceutical Drug Design Humans Inhibitory Concentration 50 Ligands Models, Chemical Pyrimidines Rats Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate Structure-Activity Relationship Time Factors

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