Ivanov C, Petkov O, Petrov P, Taskov M, Athanassova R, Tsvetkova E, Kotsev V, Lyutakov G, Nikolov G, Savov E
Chemical Pharmaceutical Research Institute, Military Medical Academy, Sofia, Bulgaria.
J Pharm Pharmacol. 1996 Mar;48(3):297-301. doi: 10.1111/j.2042-7158.1996.tb05920.x.
MX1 (N-[3-(3-(1-piperidinylmethyl)phenoxy)propyl]-hydroxyacetamide+ ++ 2-hydroxypropane-1,2,3-tricarboxylate bismuth (3+) complex) is a novel salt of the active metabolite of H2-antagonist roxatidine with a complex of bismuth with citric acid. In a model of ethanol-induced ulcers in male Wistar rats, both roxatidine and the bismuth salt reduced the number and the total length of lesions. Comparison of roxatidine and MX1 at equimolar doses of 160 mumol kg-1 showed a more potent cytoprotective effect of MX1. The potency of anti-secretory and antiacidic effects of MX1 was more than twice that of roxatidine on histamine-stimulated secretion in female Wistar pylorus-ligated rats. Microbiological tests with the reference bismuth preparation De-Nol showed prominent anti-Helicobacter properties of MX1 in-vitro. Both test compounds had similar range of MICs to Helicobacter pylori, from 4 to 64 microgram bismuth mL-1. The cytoprotective, antisecretory, anti-acidic and anti-Helicobacter properties of the new agent MX1 warrant further more extensive pharmacological and clinical trials.
MX1（N-[3-(3-(1-哌啶基甲基)苯氧基)丙基]-羟基乙酰胺+++2-羟基丙烷-1,2,3-三羧酸盐铋(3+)络合物）是H2拮抗剂罗沙替丁活性代谢产物与铋和柠檬酸形成的一种新型盐。在雄性Wistar大鼠乙醇诱导溃疡模型中，罗沙替丁和铋盐均减少了损伤的数量和总长度。在160μmol kg-1的等摩尔剂量下比较罗沙替丁和MX1，结果显示MX1具有更强的细胞保护作用。在雌性Wistar幽门结扎大鼠中，MX1的抗分泌和抗酸作用效力是罗沙替丁对组胺刺激分泌作用效力的两倍多。用参考铋制剂得乐进行的微生物学试验表明，MX1在体外具有显著的抗幽门螺杆菌特性。两种受试化合物对幽门螺杆菌的最低抑菌浓度范围相似，为4至64μg铋 mL-1。新型药物MX1的细胞保护、抗分泌、抗酸和抗幽门螺杆菌特性值得进一步进行更广泛的药理和临床试验。
