a-794282 has been researched along with Pain* in 2 studies
1 review(s) available for a-794282 and Pain
| Article | Year |
|---|---|
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
Topics: Analgesics; Animals; Humans; Pain; Peripheral Nervous System Diseases; Receptors, Metabotropic Glutamate | 2007 |
1 other study(ies) available for a-794282 and Pain
| Article | Year |
|---|---|
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
We have discovered a novel, potent, and selective triazafluorenone series of metabotropic glutamate receptor 1 (mGluR1) antagonists with efficacy in various rat pain models. Pharmacokinetic and pharmacodynamic profiles of these triazafluorenone analogs revealed that brain/plasma ratios of these mGluR1 antagonists were important to achieve efficacy in neuropathic pain models. This correlation could be used to guide our in vivo SAR (structure-activity relationship) modification. For example, compound 4a has a brain/plasma ratio of 0.34, demonstrating only moderate efficacy in neuropathic pain models. On the other hand, antagonist 4b with a brain/plasma ratio of 2.70 was fully efficacious in neuropathic pain models. Topics: Animals; Aza Compounds; Brain; Cell Line; Humans; Models, Animal; Molecular Structure; Neurons; Pain; Rats; Receptors, Metabotropic Glutamate; Structure-Activity Relationship | 2006 |