Binding Characteristics of the Muscarinic Receptor Subtype in Rabbit Pancreas
| Autor: | C. A. M. Van Ginneken, J. F. Rodrigues De Miranda, Peter H.G.M. Willems, J.J.H.H.M. De Pont, A. J. G. van Zwam |
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| Rok vydání: | 1990 |
| Předmět: |
Agonist
medicine.medical_specialty Time Factors Carbachol medicine.drug_class Tritium Binding Competitive Muscarine Internal medicine Muscarinic acetylcholine receptor medicine Animals Binding site Receptor Pancreas Pharmacology Chemistry Oxotremorine Pirenzepine Ligand (biochemistry) Receptors Muscarinic Quinuclidinyl Benzilate Dissociation constant Kinetics Endocrinology Parasympathomimetics Rabbits medicine.drug |
| Zdroj: | Journal of Receptor Research. 10:119-135 |
| ISSN: | 0197-5110 |
| Popis: | The muscarinic receptor in the rabbit pancreas was characterized with the use of the labeled ligand (3H)-(-)-quinuclidinyl-benzylate ((3H)-(-)-QNB). Specific binding of (3H)-(-)-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 (3H)-(-)-QNB binding by eight agonists like arecoline, arecaïdine-propargylester (APE) and carbachol, yielding only low affinity binding sites. The inhibition of (3H)-(-)-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. |
| Databáze: | OpenAIRE |
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