Sakurada T, Katsumata K, Yogo H, Tan-No K, Sakurada S, Kisara K
Department of Pharmacology, Tohoku College of Pharmacy, Sendai, Japan.
Neurosci Lett. 1993 Mar 19;151(2):142-5. doi: 10.1016/0304-3940(93)90006-7.
The non-peptide NK-1 receptor antagonist, CP 96,345, has been evaluated for antinociceptive activity in two chemical pain models in the mouse. CP 96,345, injected intrathecally (i.t.) 5 min prior to 2.0% formalin, produced significant antinociception in both the early and late phases of the formalin-induced paw licking procedure. Antinociception could also be observed during the late phase by treatment with CP 96,345 after formalin. In the capsaicin (CAP) test, i.t. injection of CP 96,345 produced a dose-dependent reduction of the paw-licking response at doses much less than antinociceptive doses in the formalin test. Naloxone did not affect antinociception in either test. CP 96,345 evoked a reversible deficit in motor performance as assayed by the rotarod test. The results indicate that i.t. CP 96,345 is antinociceptive in the capsaicin test at doses showing no overt behavioural effects but there is an overlap in doses producing antinociceptive and motor effects in the formalin test.
非肽类NK-1受体拮抗剂CP 96,345已在小鼠的两种化学性疼痛模型中评估了其镇痛活性。在2.0%福尔马林注射前5分钟鞘内注射CP 96,345，在福尔马林诱导的爪舔试验的早期和晚期均产生了显著的镇痛作用。在福尔马林注射后用CP 96,345治疗，在晚期也可观察到镇痛作用。在辣椒素（CAP）试验中，鞘内注射CP 96,345在远低于福尔马林试验中镇痛剂量的情况下，产生了剂量依赖性的爪舔反应降低。纳洛酮在两种试验中均不影响镇痛作用。通过转棒试验测定，CP 96,345引起了运动能力的可逆性缺陷。结果表明，鞘内注射CP 96,345在辣椒素试验中在未显示明显行为效应的剂量下具有镇痛作用，但在福尔马林试验中产生镇痛和运动效应的剂量存在重叠。
