Pharmacological activities of synthetic human cholecystokinin-33 of which tyrosine was sulfated by arylsulfotransferase.
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 x 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.
Hagiwara
M
M
Fuji Chemical Industries, Ltd., Toyama, Japan.
Ohuchi
E
E
Hongo
K
K
Oki
M
M
Nakano
M
M
Amemiya
M
M
Morikawa
T
T
Kobashi
K
K
D000818:Animals; D015239:Arylsulfotransferase / Q000378:metabolism; D002766:Cholecystokinin / Q000032:analysis / Q000494:pharmacology*; D006168:Guinea Pigs; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013431:Sulfates; D014443:Tyrosine / Q000032:analysis
D013431:Sulfates; D014443:Tyrosine; D002766:Cholecystokinin; D015239:Arylsulfotransferase