Holsapple M P, Chun A, Lagally R W, Nichols D E, Yim G K
Agents Actions. 1981 Dec;11(6-7):718-22. doi: 10.1007/BF01978795.
We have previously described the anti-inflammatory and low ulcerogenic actions of the formamidine pesticide, chlordimeform (CDM). In this study, the related basic compound, CDMI [2-(2-methyl-4-chlorophenylamino)-2-imidazoline], also demonstrated potent anti-edema (vs. carrageenin) and low ulcerogenic activity. A nonulcerogenic i.p. dose of CDMI reduced aspirin (ASA)-induced ulcers [lesion index (L.I.): 25.8 for ASA alond vs. 5.3 for ASA + i.p. CDMI]; prevented stress-induced ulcers in mice; and decreased acid secretion (by 90% in the Shay rat preparation). A mildly ulcerogenic oral dose (0.6 mmol/kg) of CDMI prevented stress ulcers, but did not reduce ASA ulcers. A nonulcerogenic oral dose (0.15 mmol/kg) of CDMI did reduce ASA ulcers (L.I.: 24.5 for ASA alone vs. 14.7 for ASA + oral CDMI). Thus, CDMI is a unique anti-inflammatory agent with additional anti-secretory and ulcer-reducing actions.
我们之前已经描述了甲脒类农药杀虫脒(CDM)的抗炎和低致溃疡作用。在本研究中,相关的碱性化合物CDMI [2-(2-甲基-4-氯苯基氨基)-2-咪唑啉]也表现出强效的抗水肿作用(与角叉菜胶相比)和低致溃疡活性。非致溃疡剂量的腹腔注射CDMI可减少阿司匹林(ASA)诱导的溃疡[损伤指数(L.I.):单独使用ASA时为25.8,而ASA +腹腔注射CDMI时为5.3];预防小鼠应激性溃疡;并减少胃酸分泌(在 Shay大鼠制备中减少90%)。轻度致溃疡的口服剂量(0.6 mmol/kg)的CDMI可预防应激性溃疡,但不能减少ASA诱导的溃疡。非致溃疡的口服剂量(0.15 mmol/kg)的CDMI确实可减少ASA诱导的溃疡(L.I.:单独使用ASA时为24.5,而ASA +口服CDMI时为14.7)。因此,CDMI是一种独特的抗炎剂,具有额外的抗分泌和减少溃疡的作用。