Interaction of gephyrotoxin and indolizidine alkaloids with the nicotinic acetylcholine receptor-ion channel complex of Torpedo electroplax.
作者： Robert S. Aronstam , John W. Daly , Thomas F. Spande , Tanjore K. Narayanan , Edson X. Albuquerque
DOI: 10.1007/BF00965950
关键词:
摘要: The interactions of eighteen natural and synthetic gephyrotoxin indolizidine alkaloids with binding sites on nicotinic acetylcholine receptor channel (AChR) complex fromTorpedo californica electric organ were investigated using two radiolabeled probes, [3H]perhydrohistrionicotoxin [3H]phencyclidine. Both gephyrotoxins indolizidines moderately active inhibitors the these probes (Ki's=0.1–20 μM), but did not interact actylcholine site. Structure-activity relationships indicate an important contribution hydrophobic to both binding. stereoconfiguration had little effect Carbamylcholine enhanced affinity certain up 6 8-fold suggesting that open or desensitized conformations AChR are favored over resting conformations.
springer.com
sci-hub.se 参考文章(26)
Robert S. Aronstam, Coleman T. King, Edson X. Albuquerque, John W. Daly, Dorothy M. Feigl, Binding of [3H]perhydrohistrionicotoxin and [3H] phencyclidine to the nicotinic receptor-ion channel complex of Torpedo electroplax: Inhibition by histrionicotoxins and derivatives Biochemical Pharmacology. ,vol. 34, pp. 3037- 3047 ,(1985) , 10.1016/0006-2952(85)90145-5
R.S. Aronstam, A.T. Eldefrawi, I.N. Pessah, J.W. Daly, E.X. Albuquerque, M.E. Eldefrawi, Regulation of [3H]perhydrohistrionicotoxin binding to Torpedo ocellata electroplax by effectors of the acetylcholine receptor. Journal of Biological Chemistry. ,vol. 256, pp. 2843- 2850 ,(1981) , 10.1016/S0021-9258(19)69691-2
W A Varanda, R S Aronstam, E X Albuquerque, J W Daly, C Souccar, Interactions of gephyrotoxin with the acetylcholine receptor-ionic channel complex. II. Enhancement of desensitization. Molecular Pharmacology. ,vol. 25, pp. 395- 400 ,(1984)
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)
J. W. Daly, Alkaloids of Neotropical Poison Frogs (Dendrobatidae) Progress in the chemistry of organic natural products. Progrès dans la chimie des substances organiques naturelles. ,vol. 41, pp. 205- 340 ,(1982) , 10.1007/978-3-7091-8656-5_6
Thierry Heidmann, Robert E. Oswald, Jean Pierre Changeux, Multiple sites of action for noncompetitive blockers on acetylcholine receptor rich membrane fragments from Torpedo marmorata Biochemistry. ,vol. 22, pp. 3112- 3127 ,(1983) , 10.1021/BI00282A014
John W. Daly, George B. Brown, Monica Mensah-Dwumah, Charles W. Myers, Classification of skin alkaloids from neotropical poison-dart frogs (Dendrobatidae). Toxicon. ,vol. 16, pp. 163- 188 ,(1978) , 10.1016/0041-0101(78)90036-3
J. W. Daly, B. Witkop, T. Tokuyama, T. Nishikawa, I. L. Karle, Gephyrotoxins, Histrionicotoxins and Pumiliotoxins from the Neotropical Frog Dendrobates histrionicus† Helvetica Chimica Acta. ,vol. 60, pp. 1128- 1140 ,(1977) , 10.1002/HLCA.19770600336
M. E. Eldefrawi, A. T. Eldefrawi, R. S. Aronstam, M. A. Maleque, J. E. Warnick, E. X. Albuquerque, [3H]Phencyclidine: a probe for the ionic channel of the nicotinic receptor. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 77, pp. 7458- 7462 ,(1980) , 10.1073/PNAS.77.12.7458
J. Changeux, A Devillers-Thiery, P Chemouilli, Acetylcholine receptor: an allosteric protein Science. ,vol. 225, pp. 1335- 1345 ,(1984) , 10.1126/SCIENCE.6382611