Interaction of antihistaminics with muscarinic receptor (III)
作者： Shin Woong Lee , Young Joo Park
DOI: 10.1007/BF02892026
关键词: Quinuclidinyl Benzilate 、 Muscarinic acetylcholine receptor 、 Biophysics 、 Chemistry 、 Histamine 、 Muscarinic antagonist 、 Carbachol 、 Muscarinic agonist 、 Dissociation constant 、 Receptor
摘要: The muscarinic antagonist 1-[benzilic 4,4′-3H]quinuclidinyl benzilate ([3H] QNB) bound to a single class of receptors with high affinity in rabbit ileal membranes. K D and B max values for [3H]QNB calculated from analysis saturation isotherms were 52.5 pM 154 fmol/mg, respectively. Chlorpheniramine (CHP), histamine H1 blocker, increased value without affecting the binding site concentrations Hill coefficient. i CHP inhibition membranes was 1.44μM pseudo-Hill coefficient close unit. In functional assay carbachol, agonist, contractile force ileum ED50 0.11μM. caused rightward shift dose-response curve carbachol. pA2 determined Schild carbachol-induced contraction 5.77 slope unity indicating competitive antagonism dissociation constant (K ) obtained experiments similar A (1.69μM) as inhibitor ileum. This result suggests that CHP, vs represents an interaction receptor physiological relevance.
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sci-hub.se 参考文章(21)
Mauricio Rocha e Silva, Abilio Antonio, Bioassay of Antihistaminic Action Springer Berlin Heidelberg. pp. 381- 437 ,(1978) , 10.1007/978-3-642-66445-8_10
A. Lewis Farr, Oliver H. Lowry, Rose J. Randall, Nira J. Rosebrough, Protein Measurement with the Folin Phenol Reagent Journal of Biological Chemistry. ,vol. 193, pp. 265- 275 ,(1951)
A. S. V. Burgen, N. J. M. Birdsall, E. C. Hulme, The binding of agonists to brain muscarinic receptors. Molecular Pharmacology. ,vol. 14, pp. 723- 736 ,(1978)
S Sorota, L P Adam, A J Pappano, Comparison of muscarinic receptor properties in hatched chick heart atrium and ventricle. Journal of Pharmacology and Experimental Therapeutics. ,vol. 236, pp. 602- 609 ,(1986)
George Scatchard, The Attractions of Proteins for Small Molecules and Ions Annals of the New York Academy of Sciences. ,vol. 51, pp. 660- 672 ,(1949) , 10.1111/J.1749-6632.1949.TB27297.X
N. J. M. Birdsall, E. C. Hulme, BIOCHEMICAL STUDIES ON MUSCARINIC ACETYLCHOLINE RECEPTORS Journal of Neurochemistry. ,vol. 27, pp. 7- 16 ,(1976) , 10.1111/J.1471-4159.1976.TB01536.X
A.S.V. Burgen, C.J. Harbird, The effect of sulphydryl block on the binding of H1-antagonists to the muscarinic receptor. British Journal of Pharmacology. ,vol. 80, pp. 600- 601 ,(1983) , 10.1111/J.1476-5381.1983.TB10048.X
N. Chand, P. Eyre, Classification and biological distribution of histamine receptor sub-types Inflammation Research. ,vol. 5, pp. 277- 295 ,(1975) , 10.1007/BF02205232
R.M. Eglen, R.L. Whiting, Competitive and non-competitive antagonism exhibited by 'selective' antagonists at atrial and ileal muscarinic receptor subtypes. British Journal of Pharmacology. ,vol. 90, pp. 701- 707 ,(1987) , 10.1111/J.1476-5381.1987.TB11223.X
D. S. Pearlman, Antihistamines: Pharmacology and Clinical Use Drugs. ,vol. 12, pp. 258- 273 ,(1976) , 10.2165/00003495-197612040-00002