The neuronal nicotinic alpha4beta2 receptor has a high maximal probability of being open.

British Journal of Pharmacology
Ping Li, Joe H Steinbach

Abstract

A fundamental property of transmitter-gated ion channels is the probability a channel will be open (P(open)) when stimulated by a concentration of agonist that elicits a maximal response. This value is critical for interpreting steady-state concentration-response relationships in terms of channel activation, and for understanding the actions of drugs that potentiate responses. We used analysis of non-stationary noise to estimate the maximal probability the nicotinic alpha4beta2 receptor is open. HEK293 cells stably transfected to express human alpha4beta2 nicotinic receptors were studied using whole-cell voltage clamp. Nicotinic agonists (acetylcholine, nicotine, cytisine and 5-iodo A-85380) were applied, and the relationship between variance of the elicited whole-cell current and mean current was analysed. The variance did not increase linearly with the mean current. For acetylcholine and nicotine the relationship between variance and mean indicates that the maximal P(open) is greater than 0.8. The number of agonist-activatable channels was estimated to be about 1000 per cell. The mean single channel conductance at -60 mV was indistinguishable when currents were elicited by acetylcholine (18 pS), nicotine (17 pS) or 5-iodo A-8...Continue Reading

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Citations

Feb 4, 2014·Biochemical Pharmacology·Roger L Papke
Sep 10, 2013·Nature Chemical Biology·Corrie J B daCostaJohn E Baenziger
Jul 24, 2010·British Journal of Pharmacology·Roger L Papke
May 29, 2016·Biochimica Et Biophysica Acta·Camila CarignanoGuillermo Spitzmaul
Nov 23, 2016·Biochimica Et Biophysica Acta. Biomembranes·Jiayin SunJohn E Baenziger
Jan 4, 2019·Recent Patents on Anti-cancer Drug Discovery·Alessia SantoroPatrizia Russo
Jan 20, 2017·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Andrew A GeorgePaul Whiteaker
Dec 19, 2014·The Journal of Biological Chemistry·Casey L CarswellJohn E Baenziger
Mar 25, 2020·Pharmacological Reviews·M J MoerkeJ L Wilkerson
Apr 30, 2019·Frontiers in Neural Circuits·Cristina ColangeloSrikanth Ramaswamy

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