Decreased Binding Affinity of Olanzapine and Clozapine for Human Muscarinic Receptors in Intact Clonal Cells in Physiological Medium
作者： Frank P Bymaster , Julie F Falcone
DOI: 10.1016/S0014-2999(00)00037-6
关键词: Internal medicine 、 Muscarinic acetylcholine receptor M1 、 Atropine 、 Acetylcholine receptor 、 Muscarinic acetylcholine receptor 、 Pharmacology 、 Clozapine 、 Endocrinology 、 Biology 、 Receptor 、 Cell culture 、 Chinese hamster ovary cell
摘要: The binding affinity of olanzapine, clozapine and atropine for muscarinic receptor subtypes in clonal Chinese hamster ovary (CHO) cell lines was compared intact cells physiological media to disrupted hypotonic buffer. olanzapine clozapine, but not atropine, (M(1)-M(5)) significantly reduced medium M(1) receptors most affected with a reduction K(i) value from 2.5 73 nM cells. These data suggest that the have been overestimated.
elsevier.com
sci-hub.se 参考文章(15)
Charles M Beasley Jr, Gary Tollefson, Pierre Tran, Winston Satterlee, Todd Sanger, Susan Hamilton, Olanzapine HGAD Study Group, Olanzapine versus placebo and haloperidol: Acute phase results of the North American double-blind olanzapine trial Neuropsychopharmacology. ,vol. 14, pp. 111- 123 ,(1996) , 10.1016/0893-133X(95)00069-P
P Seeman, H H Van Tol, Dopamine receptor pharmacology. Current opinion in neurology and neurosurgery. ,vol. 6, pp. 602- 608 ,(1993)
A DeLean, P J Munson, D Rodbard, Simultaneous analysis of families of sigmoidal curves: application to bioassay, radioligand assay, and physiological dose-response curves. American Journal of Physiology-endocrinology and Metabolism. ,vol. 235, ,(1978) , 10.1152/AJPENDO.1978.235.2.E97
M R Brann, G Lambrecht, E Mutschler, J Wess, R Tacke, F Dörje, Antagonist binding profiles of five cloned human muscarinic receptor subtypes. Journal of Pharmacology and Experimental Therapeutics. ,vol. 256, pp. 727- 733 ,(1991)
N.J.M. BIRDSALL, A.S.V. BURGEN, E.C. HULME, J.W. WELLS, THE EFFECTS OF IONS ON THE BINDING OF AGONISTS AND ANTAGONISTS TO MUSCARINIC RECEPTORS British Journal of Pharmacology. ,vol. 67, pp. 371- 377 ,(1979) , 10.1111/J.1476-5381.1979.TB08690.X
A. Schotte, P. F. M. Janssen, W. Gommeren, W. H. M. L. Luyten, P. Van Gompel, A. S. Lesage, K. De Loore, J. E. Leysen, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding Psychopharmacology. ,vol. 124, pp. 57- 73 ,(1996) , 10.1007/BF02245606
Maria C Olianas, Carlo Maullu, Pierluigi Onali, Mixed Agonist–Antagonist Properties of Clozapine at Different Human Cloned Muscarinic Receptor Subtypes Expressed in Chinese Hamster Ovary Cells Neuropsychopharmacology. ,vol. 20, pp. 263- 270 ,(1999) , 10.1016/S0893-133X(98)00048-7
Frank P Bymaster, David O Calligaro, Julie F Falcone, Richard D Marsh, Nicholas A Moore, Nicholas C Tye, Philip Seeman, David T Wong, Radioreceptor binding profile of the atypical antipsychotic olanzapine Neuropsychopharmacology. ,vol. 14, pp. 87- 96 ,(1996) , 10.1016/0893-133X(94)00129-N
Stevin H. Zorn, Shawn B. Jones, Karen M. Ward, Dane R. Liston, Clozapine is a potent and selective muscarinic M4 receptor agonist European Journal of Pharmacology. ,vol. 269, ,(1994) , 10.1016/0922-4106(94)90047-7
Cheng Yung-Chi, William H. Prusoff, Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochemical Pharmacology. ,vol. 22, pp. 3099- 3108 ,(1973) , 10.1016/0006-2952(73)90196-2