Matsuo Y, Kuwayama H, Itoh H, Seki A, Fukuda S, Kawasaki T, Hotta T, Ohsaka Y, Komatsu K
Arzneimittelforschung. 1986 Aug;36(8):1236-40.
Anti-ulcer properties of 2-(3,4-dimethoxyphenyl)-5-methylthiazolidine-4-one (KM-1146) were investigated on various experimental ulcers in comparison with cimetidine. While both KM-1146 and cimetidine at the same dose were comparative on the preventive effects of Shay- and stress-ulcers, KM-1146 was more effective against different necrotizing agents such as 0.2N NaOH and 99.5% ethanol at non-antisecretory dose. KM-1146 50 mg significantly accelerated the healing of acetic acid-induced ulcers while cimetidine 200 mg had no effect. KM-1146 increased rat gastric mucosal blood flow as measured by hydrogen gas clearance and prevented a decrease of gastric mucus gel thickness induced by water immersion restraint stress. These studies indicate that KM-1146 exerts cytoprotective action even in anti-secretory dose in addition to a significant anti-ulcer action which is comparable to cimetidine.
将2-(3,4-二甲氧基苯基)-5-甲基噻唑烷-4-酮(KM-1146)与西咪替丁相比,研究了其对各种实验性溃疡的抗溃疡特性。虽然相同剂量的KM-1146和西咪替丁对 Shay 溃疡和应激性溃疡的预防效果相当,但在非抗分泌剂量下,KM-1146对不同的坏死剂(如0.2N氢氧化钠和99.5%乙醇)更有效。50mg的KM-1146能显著加速乙酸诱导溃疡的愈合,而200mg的西咪替丁则无效。通过氢气清除率测量发现,KM-1146能增加大鼠胃黏膜血流量,并防止水浸束缚应激诱导的胃黏液凝胶厚度降低。这些研究表明,KM-1146除了具有与西咪替丁相当的显著抗溃疡作用外,即使在抗分泌剂量下也能发挥细胞保护作用。