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Decamethonium both opens and blocks endplate channels.
Open accessAbstract
Miniature endplate currents, endplate current fluctuations ("membrane noise"), and voltage-jump current relaxations were studied in voltage-clamped frog muscle fibers during decamethonium action. All three types of experiments revealed two kinetic processes controlling the opening of endplate channels, one that reflects agonist action and another that reflects local anesthetic-like blocking activity. The kinetic constants for these two steps were evaluated from measurements of the fast and slow time constants as a function of decamethonium concentration. At -130 mV membrane potential and 13 degrees, the mean open time of decamethonium-activated channels is 2.8 msec. The forward and backward rate constants for channel blocking are 1.7 X 10(7) M-1 sec-1 and 10(3) sec-1. The voltage dependencies of the channel lifetime and of the blocking equilibrium are similar to those seen with pure agonists and local anesthetics, respectively.
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Citations
Cited by
Acetylcholine Receptor: An Allosteric Protein
Changeux, J.-P., Devillers-Thiéry, A., & Chemouilli, P. (1984) · Science · doi:10.1126/science.6382611 · Cited by 623
Colquhoun, D., & Sakmann, B. (1981) · Nature · doi:10.1038/294464a0 · Cited by 353
Self-citationThe permeability of endplate channels to monovalent and divalent metal cations.
Adams, D. J., Dwyer, T. M., & Hille, B. (1980) · The Journal of general physiology · doi:10.1085/jgp.75.5.493 · Cited by 331
Heidmann, T., Bernhardt, J., Neumann, E., & Changeux, J. P. (1983) · Biochemistry · doi:10.1021/bi00292a029 · Cited by 110
The channel‐blocking action of methonium compounds on rat submandibular ganglion cells
Gurney, A. M., & Rang, H. P. (1984) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1984.tb10801.x · Cited by 100
Metadata
- Authors
- Adams, P. R., & Sakmann, B.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1978-06
- Volume
- 75
- Issue
- 6
- Pages
- 2994-2998
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2030741665
- Cited by
- 169
- References
- 0
- FWCI
- 6.27
- Type
- journal article
- Language
- en
- Open access
- green
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- Adams, P. R., & Sakmann, B. (1978). Decamethonium both opens and blocks endplate channels. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.75.6.2994
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