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日本山之内制药中央研究所,在研究组胺 H_2受体拮抗剂的过程中,发现了脒衍生物具有极强的 H_2受体拮抗怍用。1979年将氨磺酰脒基和胍基噻唑环化合,成功地合成了法马替丁(gaster)。本制剂具有较强的,持续性的抑制胃酸分泌作用,安全阈大,有抗雄性激素作用,对药物代谢酶及胆碱酯酶无破坏作用等优点。据报道,对胃酸分泌抑制作用(ED_(50)),以甲腈咪胍作为1,则 gaster 作用强度
Japan’s Yamanouchi Pharmaceutical Central Research Institute, in the study of histamine H 2 receptor antagonist process, found that amidine derivatives have a strong H 2 receptor antagonist use. In 1979, sulfamoylamino and guanidinothiazole were cyclized, and gaster was successfully synthesized. The preparation has the advantages of strong and sustained inhibitory effect on gastric acid secretion, high safety threshold, anti-androgen effect, no damaging effect on drug-metabolizing enzymes and cholinesterase, and the like. It has been reported that the inhibitory effect on gastric acid secretion (ED 50), with cetylidine as 1, the gaster action intensity