Gary Gilmour, Lisa M Broad, Keith A Wafford, Thomas Britton, Ellen M Colvin, Adam Fivush, Francois Gastambide, Brian Getman, Beverly A Heinz, Andrew P McCarthy, Lourdes Prieto, Elaine Shanks, Janice W Smith, Lorena Taboada, Dale M Edgar, Mark D Tricklebank
The demonstrated functional interaction of metabotropic glutamate 5 (mGlu₅) receptors with N-methyl-d-aspartate (NMDA) receptors has prompted speculation that their activation may offer a potential treatment for aspects of schizophrenia. Development of selective mGlu₅ agonists has been difficult, but several different positive allosteric modulator (PAM) molecules have now been identified. This study describes two novel mGlu₅ PAMs, LSN2463359 (N-(1-methylethyl)-5-(pyridin-4-ylethynyl)pyridine-2-carboxamide) and LSN2814617 [(7S)-3-tert-butyl-7-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-A]pyridine], which are useful tools for this field of research...
January 2013: Neuropharmacology