Antimuscarinic effects of chloroquine in rat pancreatic acini
Chloroquine inhibited carbachol-induced amylase release in a dose-dependent fashion in rat pancreatic acini; cholecystokinin- and bombesin-induced secretory responses were almost unchanged by the antimalarial drug. The inhibition of carbachol-induced amylase release by chloroquine was competitive in nature with a K/sub i/ of 11.7 ..mu..M. Chloroquine also inhibited (/sup 3/H)N-methylscopolamine binding to acinar muscarinic receptors. The IC/sub 50/ for chloroquine inhibition of (/sup 3/H)N-methylscopolamine binding was lower than that for carbachol or the other antimalarial drugs, quinine and quinidine. These results demonstrate that chloroquine is a muscarinic receptor antagonist in the exocrine pancreas.
- Research Organization:
- Univ. of California, San Francisco
- OSTI ID:
- 7246871
- Journal Information:
- Biochem. Biophys. Res. Commun.; (United States), Journal Name: Biochem. Biophys. Res. Commun.; (United States) Vol. 137:2; ISSN BBRCA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ALKALOIDS
AMYLASE
ANIMALS
ANTI-INFECTIVE AGENTS
ANTIMICROBIAL AGENTS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
BODY
CHEMICAL ACTIVATION
DATA
DIGESTIVE SYSTEM
DOSE-RESPONSE RELATIONSHIPS
DRUGS
ENDOCRINE GLANDS
ENZYME ACTIVITY
ENZYMES
EXPERIMENTAL DATA
GLANDS
GLYCOSYL HYDROLASES
HORMONES
HYDROLASES
INFORMATION
INHIBITION
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
NUMERICAL DATA
O-GLYCOSYL HYDROLASES
ORGANIC COMPOUNDS
ORGANS
PANCREAS
PEPTIDE HORMONES
PROTEINS
QUININE
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SECRETION
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES