Valcavi U, Caponi R, Brambilla A, Palmira M, Minoja F, Bernini F, Musanti R, Fumagalli R
Arzneimittelforschung. 1982;32(6):657-63.
9-Hydroxy-19,20-bis-nor-prostanoic acid (IBI-C83) was evaluated on gastric acid secretion and gastric lesions induced in laboratory animals by a variety of experimental conditions: compound IBI-C83 is proved effective in decreasing basal, histamine- and pentagastrin-stimulated total acid output in rats and in pentagastrin perfused dogs. The concentration of N-acetylneuraminic acid in the gastric fluid, a marker of mucus secretion, is enhanced in rats by IBI-C83. This drug prevents gastric damage induced by non-steroidal antiinflammatory compounds such as acetylsalicylic acid, indometacin and phenylbutazone, gastric ulcers following pylorus ligation, and facilitates healing of the gastric ulcers evoked by subserosal injection of acetic acid. A prominent feature of IBI-C83 is its capacity to protect the rat from gastric damage elicited by necrotizing agents such as absolute ethanol, hydrochloric acid and hypertonic saline. This property, called "cytoprotection" and common to naturally occuring prostaglandins, is independent on the antisecretory activity of IBI-C83 and is not shared, at least in the reported experimental models, by the H2-receptor antagonist cimetidine. In spite of the prostaglandin-like properties displayed in its cytoprotective activity, compound IBI-C83 does not affect cardiovascular functions, gastrointestinal transit and uterine motility.
9-羟基-19,20-双去甲前列腺酸(IBI-C83)在多种实验条件下对实验动物的胃酸分泌和胃损伤进行了评估:化合物IBI-C83被证明可有效降低大鼠基础胃酸分泌、组胺和五肽胃泌素刺激的总酸分泌,以及五肽胃泌素灌注犬的胃酸分泌。IBI-C83可提高大鼠胃液中N-乙酰神经氨酸的浓度,这是黏液分泌的一个指标。该药物可预防由非甾体类抗炎化合物如乙酰水杨酸、吲哚美辛和保泰松引起的胃损伤、幽门结扎后的胃溃疡,并促进浆膜下注射乙酸诱发的胃溃疡的愈合。IBI-C83的一个突出特点是它能够保护大鼠免受坏死剂如无水乙醇、盐酸和高渗盐水引起的胃损伤。这种特性被称为“细胞保护作用”,天然存在的前列腺素也具有这种特性,它独立于IBI-C83的抗分泌活性,并且至少在所报道的实验模型中,H2受体拮抗剂西咪替丁不具有这种特性。尽管化合物IBI-C83在其细胞保护活性中表现出类似前列腺素的特性,但它不影响心血管功能、胃肠道转运和子宫收缩。