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