Moussaoui S M, Philippe L, Le Prado N, Garret C
Rhône-Poulenc Rorer S.A., Centre de Recherche de Vitry, Alfortville, Vitry sur Sein, France.
Eur J Pharmacol. 1993 Jul 20;238(2-3):421-4. doi: 10.1016/0014-2999(93)90879-m.
RP 67580, a non-peptide NK1 receptor antagonist, inhibited in a stereoselective and dose-dependent manner plasma extravasation caused in the dura mater by intravenous injection of capsaicin in guinea-pigs and of exogenous substance P in rats (ED50 = 35 and 2.5 micrograms/kg i.v., respectively). In the two species, RP 67580 appeared to be more effective in the dura mater than in the peripheral organs. These results indicate that selective NK1 receptor antagonists could be potentially effective for the treatment of migraine headache.
RP 67580是一种非肽类NK1受体拮抗剂，能以立体选择性和剂量依赖性方式抑制豚鼠静脉注射辣椒素以及大鼠静脉注射外源性P物质所引起的硬脑膜血浆外渗（豚鼠和大鼠的半数有效剂量分别为静脉注射35微克/千克和2.5微克/千克）。在这两个物种中，RP 67580在硬脑膜中的效果似乎比在周围器官中更显著。这些结果表明，选择性NK1受体拮抗剂可能对偏头痛的治疗有潜在疗效。
