Stephen D. Hess

TL;DR: 2-methyl-6-(phenylethynyl)-pyridine is described as a potent, selective and systemically active antagonist for the metabotropic glutamate receptor subtype 5 (mGlu5) and in rat neonatal brain slices, MPEP inhibited DHPG-stimulated PI hydrolysis with a potency and selectivity similar to that observed on human mGlu receptors.

TL;DR: Cell lines expressing the human metabotropic glutamate receptor subtype 5a and hmGluR1b were used as targets in an automated high-throughput screening system that measures changes in intracellular Ca2+ ([Ca2+]i) using fluorescence detection, and the first description of highly selective, noncompetitive mGLUR5 antagonists was described.

TL;DR: (R,S)-4-phosphonophenylglycine (PPG) is described as a novel, potent, and selective agonist for group III mGluRs and protected against N-methyl-D-aspartate- and quinolinic acid-induced striatal lesions in rats and was anticonvulsive in the maximal electroshock model in mice.

TL;DR: Recombinant human mGluR5a was also stably expressed in mouse fibroblast Ltk- cells, in which the efficacy and potency of quisqualate were unchanged for more than 30 cell passages.

TL;DR: The results underscore the need for subtype-selective compounds acting at novel sites to sufficiently probe the pharmacological differences between NMDA receptor subtypes formed by different subunit combinations and suggest an ifenprodil sensitivity predicted for a population in which 51% was represented by hNMDAR(1A)2(2A)3 complexes.