Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. doi: 10.1016/j.bmcl.2006.06.078. Epub 2006 Jul 11.

Abstract

Studies of structure-activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data.

MeSH terms

  • Alkynes / chemical synthesis
  • Alkynes / chemistry*
  • Alkynes / pharmacokinetics
  • Alkynes / pharmacology*
  • Animals
  • Cross-Linking Reagents / chemistry*
  • Liver / drug effects
  • Liver / metabolism
  • Molecular Structure
  • Pyridines / chemistry*
  • Rats
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate / metabolism*
  • Structure-Activity Relationship

Substances

  • Alkynes
  • Cross-Linking Reagents
  • Grm5 protein, rat
  • Pyridines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate
  • pyridine