Rouissi N, Jukic D, D'Orléans-Juste P, Regoli D
Department of Pharmacology, Université de Sherbrooke, Québec.
Life Sci. 1993;52(13):PL103-6. doi: 10.1016/0024-3205(93)90438-9.
In rats anesthetized with urethane, substance P exerts a short-lasting hypotensive effect and stimulates salivary secretion. These effects are significantly increased and prolonged by 5 to 10 times, when substance P is administered in the presence of a mixture of peptidase inhibitors (captopril, thiorphan and phosphoramidon). Ac[Arg6,Sar9,Met(O2)11]SP(6-11), a selective NK-1 receptor agonist, shows high potency and prolonged hypotensive and sialologic effects. The effects of the NK-1 selective hexapeptide are comparable to those of substance P tested in the presence of peptidase inhibitors and are not modified by peptidase inhibitors. Ac[Arg6,Sar9,Met(O2)11]SP (6-11) is proposed as a useful tool for studying the roles and functions of NK-1 receptors in vivo, because of its stability, potency and selectivity.
在使用乌拉坦麻醉的大鼠中，P物质产生短暂的降压作用并刺激唾液分泌。当在肽酶抑制剂（卡托普利、硫氧还蛋白和磷酰胺脒）混合物存在的情况下给予P物质时，这些作用会显著增强并延长5至10倍。Ac[Arg6,Sar9,Met(O2)11]SP(6-11)，一种选择性NK-1受体激动剂，显示出高效力以及持久的降压和唾液分泌作用。NK-1选择性六肽的作用与在肽酶抑制剂存在下测试的P物质的作用相当，并且不受肽酶抑制剂的影响。由于其稳定性、效力和选择性，Ac[Arg6,Sar9,Met(O2)11]SP (6-11)被认为是研究体内NK-1受体的作用和功能的有用工具。
