Ivanova E A, Zolotov N N, Voronina T A
Zakusov Institute of Pharmacology, Moscow, Russia.
Biomed Khim. 2020 Sep;66(5):423-426. doi: 10.18097/PBMC20206605423.
A selective prolyl endopeptidase (PEP) inhibitor benzyloxycarbonyl-prolyl-prolinal (IC50 = 1,61±0,12 nmol/l) and a nonselective PEP inhibitor benzyloxycarbonyl-methionyl-cyanopyrrolidine (IC50 = 2,01±0,14 nmol/l) exhibit a comparable antiexudative effect at single doses of 2 mg/kg and 5 mg/kg (intraperitoneally) in outbred mice with peritonitis induced by 1% acetic acid. However, only benzyloxycarbonyl-methionyl-cyanopyrrolidine at a dose of 5 mg/kg reduces acetic acid induced pain in animals.
一种选择性脯氨酰内肽酶（PEP）抑制剂苄氧羰基 - 脯氨酰 - 脯氨醛（IC50 = 1.61±0.12 nmol/L）和一种非选择性PEP抑制剂苄氧羰基 - 甲硫氨酰 - 氰基吡咯烷（IC50 = 2.01±0.14 nmol/L），在以2mg/kg和5mg/kg（腹腔注射）的单剂量给药时，对由1%乙酸诱导腹膜炎的远交系小鼠表现出相当的抗渗出作用。然而，只有剂量为5mg/kg的苄氧羰基 - 甲硫氨酰 - 氰基吡咯烷能减轻动物体内乙酸诱导的疼痛。
