Jeffrey Kedrowski

Publications (2)4.8 Total impact

• Article: Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.

  Sameer Sharma, Jeffrey Kedrowski, Jerri M Rook, Randy L Smith, Carrie K Jones, Alice L Rodriguez, P Jeffrey Conn, Craig W Lindsley
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  ABSTRACT: We describe the synthesis and SAR of a series of analogues of the mGlu(5) partial antagonist 5-(phenylethynyl)pyrimidine. New molecular switches are identified that modulate the pharmacological activity of the lead compound. Slight structural modifications around the proximal pyrimidine ring change activity of the partial antagonist lead to that of potent and selective full negative allosteric modulators and positive allosteric modulators, which demonstrate in vivo efficacy in rodent models for anxiolytic and antipsychotic activity, respectively.
  Journal of Medicinal Chemistry 07/2009; 52(14):4103-6. · 4.80 Impact Factor
• Article: Discovery of Molecular Switches That Modulate Modes of Metabotropic Glutamate Receptor Subtype 5 (mGlu 5 ) Pharmacology in Vitro and in Vivo within a Series of Functionalized, Regioisomeric 2- and 5-(Phenylethynyl)pyrimidines

  Sameer Sharma, Jeffrey Kedrowski, Jerri M. Rook, Randy L. Smith, Carrie K. Jones, Alice L. Rodriguez, P. Jeffrey Conn, Craig W. Lindsley
  Journal of Medicinal Chemistry - J MED CHEM. 01/2009; 52(14):4103-4106.