Binding characteristics of the muscarinic receptor subtype in rabbit pancreas

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Journal of Receptor Research; (USA)

DOI:https://doi.org/10.3109/10799899009064661· OSTI ID:6152153

van Zwam, A J; Willems, P H; Rodrigues de Miranda, J F; de Pont, J J; van Ginneken, C A ^[1]

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1. Catholic Univ. of Nijmegen (Netherlands)

The muscarinic receptor in the rabbit pancreas was characterized with the use of the labeled ligand ({sup 3}H)-(-)-quinuclidinyl-benzylate (({sup 3}H)-(-)-QNB). Specific binding of ({sup 3}H)-(-)-QNB to pancreatic acini was found to be reversible and of high affinity, with an equilibrium dissociation constant (KD) of 68 pmol/l and a receptor density (RT) of 170 fmol/mg protein. Agonist binding behaviour was investigated by displacement of ({sup 3}H)-(-)-QNB binding by eight agonists like arecoline, arecadine-propargylester (APE) and carbachol, yielding only low affinity binding sites. The inhibition of ({sup 3}H)-(-)-QNB binding by the selective antagonists pirenzepine, hexahydrosiladifenidol (HHSiD) and (11-(2-(diethyl-amino)-methyl-1-piperidinyl)acetyl)-5,11-dihydro-6H-pyr ido (2,3-b) (1,4) benzodiazepin-6-one (AF-DX 116) confirmed the M3 nature of the rabbit pancreatic receptor.

• OSTI ID: 6152153
• Journal Information: Journal of Receptor Research; (USA), Vol. 10:1-2; ISSN 0197-5110
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PARASYMPATHOMIMETICS
RECEPTORS
CHEMICAL COMPOSITION
BIOCHEMICAL REACTION KINETICS
PANCREAS
RABBITS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
DIGESTIVE SYSTEM
DRUGS
ENDOCRINE GLANDS
GLANDS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANS
PROTEINS
REACTION KINETICS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques