Different antagonist binding properties of rat pancreatic and cardiac muscarinic receptors
Journal Article
·
· Life Sci.; (United States)
The antagonist binding properties of rat pancreatic and cardiac muscarinic receptors were compared. In both tissues pirenzepine (PZ) had a low affinity for muscarinic receptors labelled by (/sup 3/H)N-methylscopolamine ((/sup 3/)NMS) (K/sub D/ values of 140 and 280nM, respectively, in pancreatic and cardiac homogenates). The binding properties of pancreatic and cardiac receptors were, however, markedly different. This was indicated by different affinities for dicyclomine, (11-(/(2-((diethylamino)-methyl)-1-piperidinyl/acetyl)-5, 11-dihydro-6H-pyrido(2,3-b)(1,4) benzodiazepin-6-on)(AFDX-116), 4-diphenylacetoxy-N-methyl-piperidine methobromide (4-DAMP) and hexahydrosiladifenidol (HHSiD). Pancreatic and cardiac muscarinic receptros also showed different (/sup 3/H)NMS association and dissociation rates. These results support the concept of M2 receptor subtypes have different binding kinetic properties. 20 references, 3 figures, 1 table.
- Research Organization:
- Universite Libre de Bruxelles, Brussels, Belgium
- OSTI ID:
- 5564573
- Journal Information:
- Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 41:19; ISSN LIFSA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ALCOHOLS
AMINES
AMMONIUM COMPOUNDS
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CARDIOVASCULAR SYSTEM
CHEMICAL PROPERTIES
CHOLINE
COMPARATIVE EVALUATIONS
DATA
DIGESTIVE SYSTEM
DRUGS
ENDOCRINE GLANDS
EXPERIMENTAL DATA
GLANDS
HEART
HYDROXY COMPOUNDS
INFORMATION
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIPOTROPIC FACTORS
MAMMALS
MEMBRANE PROTEINS
NUMERICAL DATA
ORGANIC COMPOUNDS
ORGANS
PANCREAS
PROTEINS
QUATERNARY COMPOUNDS
RATS
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ALCOHOLS
AMINES
AMMONIUM COMPOUNDS
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CARDIOVASCULAR SYSTEM
CHEMICAL PROPERTIES
CHOLINE
COMPARATIVE EVALUATIONS
DATA
DIGESTIVE SYSTEM
DRUGS
ENDOCRINE GLANDS
EXPERIMENTAL DATA
GLANDS
HEART
HYDROXY COMPOUNDS
INFORMATION
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIPOTROPIC FACTORS
MAMMALS
MEMBRANE PROTEINS
NUMERICAL DATA
ORGANIC COMPOUNDS
ORGANS
PANCREAS
PROTEINS
QUATERNARY COMPOUNDS
RATS
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES