The effect of the cholecystokinin receptor antagonist MK-329 on meal-stimulated pancreaticobiliary output in humans

1. A double-blind study was undertaken to determine whether the infusion of bombesin inhibits the intake of a carbohydrate-rich meal, consumed 15 min after a 300 ml banana shake, in nine lean healthy subjects and whether the possible inhibition of food intake by bombesin is mediated by cholecystokinin. 2. The amount of food eaten during infusion of bombesin (267 ±60 g) and bombesin combined with the cholecystokinin-receptor antagonist loxiglumide (269±39g) was slightly (P = 0.09) less than during saline infusion (384 ± 40 g). In addition, preprandial feelings of hunger were significantly less during infusion of both bombesin and bombesin combined with loxiglumide. 3. In conclusion, infusion of bombesin tends to inhibit the intake of a carbohydrate-rich meal after a preload by a cholecystokinin-independent mechanism.

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Effect of the cholecystokinin-receptor antagonist lorglumide on pancreatic enzyme secretion stimulated by bombesin, food, and caerulein, giving similar plasma cholecystokinin concentrations in the dog.

Gut ◽

10.1136/gut.32.2.215 ◽

1991 ◽

Vol 32 (2) ◽

pp. 215-219 ◽

Cited By ~ 6

Author(s):

A J de Jong ◽

M V Singer ◽

J B Jansen ◽

W Niebel ◽

L C Rovati ◽

...

Keyword(s):

Receptor Antagonist ◽

Pancreatic Enzyme ◽

Enzyme Secretion ◽

Cholecystokinin Receptor ◽

Plasma Cholecystokinin ◽

Pancreatic Enzyme Secretion

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Physiological role of cholecystokinin on postprandial insulin secretion and gastric meal emptying in man. Studies with the cholecystokinin receptor antagonist loxiglumide

Diabetologia ◽

10.1007/bf00401517 ◽

1991 ◽

Vol 34 (10) ◽

pp. 721-726 ◽

Cited By ~ 33

Author(s):

M. Fried ◽

W. Schwizer ◽

C. Beglinger ◽

U. Keller ◽

J. B. Jansen ◽

...

Keyword(s):

Insulin Secretion ◽

Receptor Antagonist ◽

Physiological Role ◽

Cholecystokinin Receptor ◽

Postprandial Insulin

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Effect of a New Cholecystokinin Receptor Antagonist (KSG 504) on the Early Stage of the Healing Process in Acute Pancreatitis Induced in Rats by the Closed Duodenal Loop Technique

Pancreas ◽

10.1097/00006676-199407000-00013 ◽

1994 ◽

Vol 9 (4) ◽

pp. 501-507 ◽

Cited By ~ 6

Author(s):

Sin-soo Ha ◽

Katsusuke Satake ◽

Akihito Hiura ◽

Michio Sowa ◽

Hideki Nishiwaki

Keyword(s):

Acute Pancreatitis ◽

Receptor Antagonist ◽

Early Stage ◽

Healing Process ◽

Cholecystokinin Receptor ◽

Closed Duodenal Loop ◽

Loop Technique

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Abstract 2728: Cholecystokinin receptor antagonist proglumide reverses nonalcoholic steatohepatitis and prevents hepatocellular carcinoma

10.1158/1538-7445.sabcs18-2728 ◽

2019 ◽

Author(s):

Martha D. Gay ◽

Victor Ciofoaia ◽

Sandeep Nadella ◽

Hong Cao ◽

Matthew Huber ◽

...

Keyword(s):

Hepatocellular Carcinoma ◽

Receptor Antagonist ◽

Nonalcoholic Steatohepatitis ◽

Cholecystokinin Receptor

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Role of sulfate ester in influencing biologic activity of cholecystokinin-related peptides

AJP Gastrointestinal and Liver Physiology ◽

10.1152/ajpgi.1987.252.2.g178 ◽

1987 ◽

Vol 252 (2) ◽

pp. G178-G181 ◽

Cited By ~ 2

Author(s):

R. Vinayek ◽

R. T. Jensen ◽

J. D. Gardner

Keyword(s):

Guinea Pig ◽

Receptor Antagonist ◽

Partial Agonist ◽

Tyrosine Residue ◽

Sulfate Ester ◽

Rat Pancreas ◽

Cck Receptors ◽

Cholecystokinin Receptor ◽

Cholecystokinin Receptors

In dispersed acini from guinea pig, mouse, or rat pancreas cholecystokinin-(27-33) is a full agonist, and removing the sulfate ester from the tyrosine residue in position 27 caused a 100- to 300-fold decrease in potency with no change in efficacy. In dispersed acini from mouse or rat pancreas, cholecystokinin-(27-32)-NH2 is a partial agonist, and removing the sulfate ester from the tyrosine in position 27 abolished the efficacy. The desulfated peptide was able, however, to interact with CCK receptors with a potency that was threefold less than that of cholecystokinin-(27-32)-NH2 and therefore functioned as a cholecystokinin receptor antagonist. In dispersed acini from guinea pig pancreas cholecystokinin-(27-32)-NH2 is a cholecystokinin receptor antagonist. Removing the sulfate ester from the tyrosine residue in position 27 of cholecystokinin(27-32)-NH2 caused a fourfold decrease in potency but did not abolish the ability of the peptide to interact with cholecystokinin receptors; therefore, desulfated cholecystokinin-(27-32)-NH2 functioned as a cholecystokinin receptor antagonist.

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