In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists

The SAR of a series of novel pyrido[3,4-d]pyramid-4-ylamine mGluR1 antagonists is described. The multiple of the unbound Ki in cerebrospinal fluid necessary to give morphine like analgesic effects in an electromyograph pinch model in rodents is determined and the effect of structure on CNS penetration examined.

Graphical abstractSAR and CNS penetration of a series of novel mgluR1 antagonists is described. The multiple of the unbound Ki in cerebrospinal fluid necessary to give morphine like analgesic effects in an electromyograph pinch model in rodents is given.Figure optionsDownload full-size imageDownload as PowerPoint slide