Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor
Copyright policy )Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor
We have identified and synthesized a series of biphenyl-carboxylic acid indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency and the brain to plasma ratio of the initial lead led to the discovery of 5 and 23 (EC50=111 and 5 nM, respectively).
- General Atomics (United States) United States
Brain Chemistry, Biphenyl Compounds, Receptors, Metabotropic Glutamate, Rats, Structure-Activity Relationship, Allosteric Regulation, Guanosine 5'-O-(3-Thiotriphosphate), Indans, Schizophrenia, Animals, Humans, Tissue Distribution
Brain Chemistry, Biphenyl Compounds, Receptors, Metabotropic Glutamate, Rats, Structure-Activity Relationship, Allosteric Regulation, Guanosine 5'-O-(3-Thiotriphosphate), Indans, Schizophrenia, Animals, Humans, Tissue Distribution
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