CCK Heptapeptide Analogs: Effect of Conformational Restrictions and Standard Modifications on Selectivity and Activity at CCK-A and CCK-B Receptors

Cholecystokinin (CCK) is a peptide hormone involved in the regulation of gall bladder contraction, pancreatic enzyme secretion, and gastric emptying. Exogenous CCK or its close analogs suppress feeding in a number of species, including man, and endogenous CCK may have a role in the normal satiety re...

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Bibliographic Details
Main Authors: Holladay, Mark W, Bennett, Michael J, Tufano, Michael D, Lin, C. W, Witte, David G
Format: Report
Language:English
Subjects:
ANOREXIA
APPETITE
Biochemistry
CHEMICAL ANALOGS
Cholecystokinin
Coomponent Reports
GALLBLADDER
HEPTANES
PANCREATIC HORMONES
PEPTIDES
PHARMACOLOGICAL ANTAGONISTS
Pharmacology
RECEPTOR SITES(PHYSIOLOGY)
SUPPRESSORS
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Summary:Cholecystokinin (CCK) is a peptide hormone involved in the regulation of gall bladder contraction, pancreatic enzyme secretion, and gastric emptying. Exogenous CCK or its close analogs suppress feeding in a number of species, including man, and endogenous CCK may have a role in the normal satiety response. As part of our effort toward development of anorectic agents based on CCK, we investigated the structural and conformational requirements for activity at CCK-A and CCK-B receptor subtypes.