
pmid: 21757343
A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vitro potencies and brain penetration in rodents.
Models, Molecular, Pyrrolidines, Dose-Response Relationship, Drug, Molecular Structure, Pyridines, Receptor, Metabotropic Glutamate 5, Stereoisomerism, Receptors, Metabotropic Glutamate, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, HEK293 Cells, Animals, Humans
Models, Molecular, Pyrrolidines, Dose-Response Relationship, Drug, Molecular Structure, Pyridines, Receptor, Metabotropic Glutamate 5, Stereoisomerism, Receptors, Metabotropic Glutamate, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, HEK293 Cells, Animals, Humans
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