论文部分内容阅读
本世纪六十年代后期人们发现,前列腺素E(PGE)等对动物或人的胃液分泌有强烈抑制作用,随后又相继发现动物的胃粘膜含有高浓度的PG 和非甾体抗炎药(NSAID)引起的消化道损伤与其抑制PG 合成有关,因而引起人们对PG 用于治疗消化性溃疡可能性的兴趣。但由于天然存在的PG 可被机体组织内的酶迅速代谢灭活,口服无效,注射也作用短暂,且由于作用选择性不高,不良反应多,而妨碍其作为药物使用于临床。嗣后,针对PG 的代谢特点合成了许多PGE 衍生物,发现某些衍生物不仅口服有效,且抑制胃酸分泌的作用强度超过
The late sixties of the century found that prostaglandin E (PGE) and other animal or human gastric secretion has a strong inhibitory effect, followed by the animals have been found in the gastric mucosa containing high concentrations of PG and non-steroidal anti-inflammatory drugs (NSAID ) Of gastrointestinal damage caused by its inhibition of PG synthesis, and thus lead to the use of PG for the treatment of peptic ulcer interest. However, the naturally occurring PG can be rapidly metabolized in vivo and inactivated by the enzyme in the body tissue. Oral administration is ineffective and the injection also has a short acting effect. Due to its low selectivity and adverse reactions, PG is prevented from being used clinically as a medicine. Subsequently, a number of PGE derivatives were synthesized based on the metabolic characteristics of PG. Some derivatives were found not only to be orally effective but also to inhibit gastric acid secretion more than