Ho R S, Kelly L A, Gogerty J H, Trapold J H, Timms A R
Arch Int Pharmacodyn Ther. 1977 Oct;229(2):337-50.
The present studies were undertaken to define the effects of 3-phenylpropylaminoguanidine-HCl (SaH 43-522 or 43-522) on glucose active transport in the gastrointestinal tract. A comparison with phenformin (DBI) was made in certain studies. SaH 43-522 is 2 to 3 times more potent than DBI with regard to its inhibitory effect on glucose active transport in the gastrointestinal tract of rats. The activity lasts for 5 hr after oral administration. SaH 43-522 also inhibits intestinal glucose absorption in the hamster, guinea-pig, dog, and monkey in either in vitro or in vivo systems. SaH 43-522 differs from DBI in that when glucose active transport is studied in vitro by adding drug into the incubation fluid, DBI is active only when the drug is present in the incubation fluids on both the mucosal and serosal sides, whereas SaH 43-522 is active in inhibiting intestinal glucose active transport when the drug is present in mucosal fluid only.
本研究旨在确定3-苯基丙基氨基胍盐酸盐(SaH 43-522或43-522)对胃肠道葡萄糖主动转运的影响。在某些研究中与苯乙双胍(DBI)进行了比较。就其对大鼠胃肠道葡萄糖主动转运的抑制作用而言,SaH 43-522的效力比DBI强2至3倍。口服给药后,该活性持续5小时。在体外或体内系统中,SaH 43-522也能抑制仓鼠、豚鼠、狗和猴子的肠道葡萄糖吸收。SaH 43-522与DBI的不同之处在于,当通过向孵育液中添加药物在体外研究葡萄糖主动转运时,DBI只有在孵育液的黏膜侧和浆膜侧都存在药物时才具有活性,而SaH 43-522仅在黏膜液中存在药物时就能有效抑制肠道葡萄糖主动转运。