Wang L D, Sowell J W, Freeman J J, Kosh J W
J Pharm Sci. 1981 Jun;70(6):699-701. doi: 10.1002/jps.2600700637.
A series of 2-(2-alkylaminoalkylamido)-3-carbamyl-4-methyl-5-benzylpyrroles was synthesized and screened for vasoactivity. The compounds were administered intraperitoneally as a suspension to approximate the oral route of administration and intravenously when solubilization could be affected with suitable solvents. The most active compound following intravenous or intraperitoneal administration lowered blood pressure 73 and 35.5 mm Hg at doses of 4 mg/kg iv and 100mg/kg ip, respectively. It also exhibited the longest duration of vasodepressor activity (25 min). Several other compounds exhibited vasodepressor activity following intraperitoneal administration. Several hydrochloride salts appeared to be more potent vasoactive agents than the corresponding bases.
合成了一系列2-(2-烷基氨基烷基酰胺基)-3-氨甲酰基-4-甲基-5-苄基吡咯，并对其血管活性进行了筛选。这些化合物以悬浮液形式腹腔注射以模拟口服给药途径，当可用合适溶剂溶解时则静脉注射。静脉注射或腹腔注射后活性最强的化合物，在静脉注射剂量为4mg/kg和腹腔注射剂量为100mg/kg时，分别使血压降低73和35.5毫米汞柱。它还表现出最长的血管减压活性持续时间（25分钟）。其他几种化合物腹腔注射后也表现出血管减压活性。几种盐酸盐似乎比相应的碱是更有效的血管活性剂。
