n-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide and Psychotic-Disorders

n-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide has been researched along with Psychotic-Disorders* in 1 studies

Other Studies

1 other study(ies) available for n-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide and Psychotic-Disorders

ArticleYear
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
    Bioorganic & medicinal chemistry letters, 2012, Oct-15, Volume: 22, Issue:20

    We report the optimization of a series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on a simple acyclic ether series. Modifications led to a gain of MPEP site interaction through incorporation of a chiral amide in conjunction with a nicotinamide core. A highly potent PAM, 8v (VU0404251), was shown to be efficacious in a rodent model of psychosis. These studies suggest that potent PAMs within topologically similar chemotypes can be developed to preferentially interact or not interact with the MPEP allosteric binding site.

    Topics: Allosteric Regulation; Allosteric Site; Animals; Antipsychotic Agents; Ethers; Humans; Niacinamide; Psychotic Disorders; Rats; Receptor, Metabotropic Glutamate 5; Receptors, Metabotropic Glutamate; Structure-Activity Relationship

2012