| References: |
Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil. Ongoing inflammatory nociception, observed as hindpaw weight-bearing deficits after Freund's adjuvant injection, was also completely reversed by NS11394. Likewise, hindpaw mechanical allodynia was fully reversed by NS11394 in two rat models of peripheral neuropathic pain. Importantly, NS11394-mediated antinociception occurred at doses 20 to 40-fold lower than those inducing minor sedative or ataxic impairments. In contrast, putative antinociception associated with administration of either diazepam, zolpidem, or gaboxadol only occurred at doses producing intolerable side effects, whereas bretazenil was completely inactive despite minor influences on motoric function. In electrophysiological studies, NS11394 selectively attenuated spinal nociceptive reflexes and C-fiber-mediated wind-up in vitro pointing to involvement of a spinal site of action. The robust therapeutic window seen with NS11394 in animals suggests that compounds with this in vitro selectivity profile could have potential benefit in clinical treatment of pain in humans. For the detailed information of NS11394, the solubility of NS11394 in water, the solubility of NS11394 in DMSO, the solubility of NS11394 in PBS buffer, the animal experiment (test) of NS11394, the cell expriment (test) of NS11394, the in vivo, in vitro and clinical trial test of NS11394, the EC50, IC50,and affinity,of NS11394, For the detailed information of NS11394, the solubility of NS11394 in water, the solubility of NS11394 in DMSO, the solubility of NS11394 in PBS buffer, the animal experiment (test) of NS11394, the cell expriment (test) of NS11394, the in vivo, in vitro and clinical trial test of NS11394, the EC50, IC50,and affinity,of NS11394, Please contact DC Chemicals. |
