Binding characteristics of the muscarinic receptor subtype in rabbit pancreas

Journal Article · Sun Dec 31 23:00:00 EST 1989 · 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), Journal Name: Journal of Receptor Research; (USA) Vol. 10:1-2; ISSN 0197-5110; ISSN JRERD
• Country of Publication: United States
• Language: English

Related Subjects

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