3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
Copyright policy )3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
We have identified and synthesized a brain penetrant propanoic acid as an allosteric potentiator of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency, level of potentiation and brain penetration led to the discovery of 8 (EC50=1200 nM, 77% potentiation, 119% brain/plasma in rat, 20 mpk i.p., brain level of 5700 nM).
- General Atomics (United States) United States
Phenyl Ethers, Molecular Conformation, Brain, Receptors, Metabotropic Glutamate, Rats, Kinetics, Structure-Activity Relationship, Allosteric Regulation, Guanosine 5'-O-(3-Thiotriphosphate), Butanes, Animals, Propionates
Phenyl Ethers, Molecular Conformation, Brain, Receptors, Metabotropic Glutamate, Rats, Kinetics, Structure-Activity Relationship, Allosteric Regulation, Guanosine 5'-O-(3-Thiotriphosphate), Butanes, Animals, Propionates
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