Pharmacological Activities of Synthetic Human Cholecystokinin-33 of Which Tyrosine Was Sulfated by Arylsulfotransferase

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The pharmacological activities of synthetic human CCK-33,in which a tyrosine molecule was sulfated by arylsulfotransferase, were investigated in the rat and the guinea-pig. The activities were compared with those of non-sulfated CCK-33 (CCK-33NS), CCK-8 and CCK-4. CCK-33 was about 100 fold more potent than non-sulfated CCK-33(CCK-33NS)but was about 20 fold less potent than CCK-8 in the contraction of the isolated gallbladder of the guinea-pig. In rat pancreatic secretion, intravenous CCK-33 and CCK-8 showed almost the same activity. The potency of each was about 1000 fold more than the individual potency of CCK-33NS, non-sulfated CCK-8 (CCK-8NS) and CCK4. There were no significant differences in gastric acid stimulatory activities among CCK-33,CCK-8,CCK-4,but the activities of CCK-33NS and CCK-8NS were less than those of CCK-33 and CCK-8,respectively. CCK-33 and CCK-8 produced a reduction in the intake of powder chow in doses of 10^<-8> and 3×10^<-8>mol/kg i.p., but CCK-33NS, CCK-8NS and CCK-4 did not. In conclusion, the activities of synthetic human CCK-33 are almost the same as those of CCK-8 on exocrine pancreatic secretion, gastric acid secretion and food intake, but less than CCK-8 on isolated gallbladder contraction.
公益社団法人日本薬学会の論文
1990-05-25