Skip to main content
British Journal of Pharmacology and Chemotherapy logoLink to British Journal of Pharmacology and Chemotherapy
. 1962 Aug;19(1):198–218. doi: 10.1111/j.1476-5381.1962.tb01440.x

Triethylcholine compared with other substances affecting neuromuscular transmission

W C Bowman, B A Hemsworth, M J Rand
PMCID: PMC1482233  PMID: 13872106

Abstract

Triethylcholine (triethyl-2-hydroxyethyl ammonium) has been compared, in its actions on neuromuscular transmission, with the motor end-plate blocking drugs tubocurarine and decamethonium, with the anticholinesterase neostigmine, and with the closely related drug tetraethylammonium. The experiments were carried out on conscious rabbits and mice, on the tibialis anterior muscle of cats under chloralose anaesthesia and on the isolated phrenic nerve-diaphragm preparation of the rat. Anticholinesterase activity was determined manometrically using the Warburg apparatus. Triethylcholine possessed a slight curare-like action, but this effect was shown to be too weak and transient to contribute to the slowly developing and long-lasting transmission failure which occurs selectively in frequently excited nervemuscle preparations and in exercised conscious animals. It was confirmed that the site of the blocking action of triethylcholine was pre-junctional. Triethylcholine often produced a slight potentiation of the contractions before blocking them. This effect was not due to a depolarizing or an anticholinesterase action, and it was concluded that the slight initial facilitating action of triethylcholine on neuromuscular transmission was due to an increase in the quantity of acetylcholine released by the nerve impulse. Tetraethylammonium was much more powerful than triethylcholine in this respect. The pre-junctional transmission failure produced by triethylcholine could not be explained simply on the basis that an initial excessive release led to exhaustion of transmitter.

Full text

PDF
198

Images in this article

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. ALDRIDGE W. N. Some properties of specific cholinesterase with particular reference to the mechanism of inhibition by diethyl p-nitrophenyl thiophosphate (E 605) and analogues. Biochem J. 1950 Apr;46(4):451–460. doi: 10.1042/bj0460451. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. ATKINSON W. J., Jr Effect of tetraethylammonium chloride on mammalian skeletal muscle action. Am J Physiol. 1952 Feb;168(2):442–445. doi: 10.1152/ajplegacy.1952.168.2.442. [DOI] [PubMed] [Google Scholar]
  3. BLIGH J. The level of free choline in plasma. J Physiol. 1952 Jun;117(2):234–240. doi: 10.1113/jphysiol.1952.sp004743. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. BOWMAN W. C., RAND M. J. Actions of triethylcholine on neuromuscular transmission. Br J Pharmacol Chemother. 1961 Oct;17:176–195. doi: 10.1111/j.1476-5381.1961.tb01278.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. BURGEN A. S. V., DICKENS F., ZATMAN L. J. The action of botulinum toxin on the neuro-muscular junction. J Physiol. 1949 Aug;109(1-2):10–24. doi: 10.1113/jphysiol.1949.sp004364. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. BURGEN A. S., BURKE G., DESBARATSSCHONBAUM M. L. The specificity of brain choline acetylase. Br J Pharmacol Chemother. 1956 Sep;11(3):308–312. doi: 10.1111/j.1476-5381.1956.tb01071.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. BURNS B. D., PATON W. D. M. Depolarization of the motor end-plate by decamethonium and acetylcholine. J Physiol. 1951 Sep;115(1):41–73. doi: 10.1113/jphysiol.1951.sp004652. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Bacq Z. M., Brown G. L. Pharmacological experiments on mammalian voluntary muscle, in relation to the theory of chemical transmission. J Physiol. 1937 Feb 19;89(1):45–60. doi: 10.1113/jphysiol.1937.sp003461. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Briscoe G. Changes in muscle contraction curves produced by drugs of the eserine and curarine groups. J Physiol. 1938 Aug 15;93(3):194–205. doi: 10.1113/jphysiol.1938.sp003635. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Brown G. L. Action potentials of normal mammalian muscle. Effects of acetylcholine and eserine. J Physiol. 1937 Mar 5;89(2):220–237. doi: 10.1113/jphysiol.1937.sp003474. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. HOFMANN W. W., FEIGEN G. A., GENTHER G. H. Hemicholinium no. 3 and mammalian neuromuscular transmission. Nature. 1962 May 19;194:654–656. doi: 10.1038/194654a0. [DOI] [PubMed] [Google Scholar]
  12. HUTTER O. F. Effect of choline on neuromuscular transmission in the cat. J Physiol. 1952 Jun;117(2):241–250. doi: 10.1113/jphysiol.1952.sp004744. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. JEPSON R. P., SIMEONE F. A., LYNN R. B. Effects of certain autonomic blocking agents on striated muscle function. Am J Physiol. 1953 Apr;173(1):70–74. doi: 10.1152/ajplegacy.1953.173.1.70. [DOI] [PubMed] [Google Scholar]
  14. KOKETSU K. Action of tetraethylammonium chloride on neuromuscular transmission in frogs. Am J Physiol. 1958 Apr;193(1):213–218. doi: 10.1152/ajplegacy.1958.193.1.213. [DOI] [PubMed] [Google Scholar]
  15. KRNJEVIC K., MILEDI R. Failure of neuromuscular propagation in rats. J Physiol. 1958 Mar 11;140(3):440–461. [PMC free article] [PubMed] [Google Scholar]
  16. LAURENCE D. R., WEBSTER R. A. Activity of the triethyl analogue of choline in suppressing experimental tetanus. Lancet. 1961 Mar 4;1(7175):481–482. doi: 10.1016/s0140-6736(61)90062-9. [DOI] [PubMed] [Google Scholar]
  17. MARTIN A. R., ORKAND R. K. Postsynaptic effects of HC-3 at the neuromuscular junction of the frog. Can J Biochem Physiol. 1961 Feb;39:343–349. doi: 10.1139/o61-034. [DOI] [PubMed] [Google Scholar]
  18. MCEWEN L. M. The effect on the isolated rabbit heart of vagal stimulation and its modification by cocaine, hexamethonium and ouabain. J Physiol. 1956 Mar 28;131(3):678–689. doi: 10.1113/jphysiol.1956.sp005493. [DOI] [PMC free article] [PubMed] [Google Scholar]
  19. PRESTON J. B., VAN MAANEN E. F. Effects of frequency of stimulation on the paralyzing dose of neuromuscular blocking agents. J Pharmacol Exp Ther. 1953 Feb;107(2):165–171. [PubMed] [Google Scholar]
  20. REITZEL N. L., LONG J. P. The neuromuscular blocking properties of alpha, alpha, dimethylethanolamino 4,4' biacetophenone (hemicholinium). Arch Int Pharmacodyn Ther. 1959 Mar 1;119(1-2):20–30. [PubMed] [Google Scholar]
  21. ROBERTS D. V. Neuromcuscular activity of the triethyl analogue of choline in the frog. J Physiol. 1962 Jan;160:94–105. doi: 10.1113/jphysiol.1962.sp006836. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. STOVNER J. The anticurare activity of tetraethylammonium (TEA). Acta Pharmacol Toxicol (Copenh) 1958;14(4):317–332. [PubMed] [Google Scholar]
  23. STOVNER J. The effect of low calcium and of tetraethylammonium (TEA) on the rat diaphragm. Acta Physiol Scand. 1957 Oct 10;40(2-3):285–296. doi: 10.1111/j.1748-1716.1957.tb01497.x. [DOI] [PubMed] [Google Scholar]
  24. THIES R. E., BROOKS V. B. Postsynaptic neuromuscular block produced by hemicholinium no. 3. Fed Proc. 1961 Jul;20:569–578. [PubMed] [Google Scholar]
  25. WERNER G. Neuromuscular facilitation and antidromic discharges in motor nerves: their relation to activity in motor nerve terminals. J Neurophysiol. 1960 Mar;23:171–187. doi: 10.1152/jn.1960.23.2.171. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology and Chemotherapy are provided here courtesy of The British Pharmacological Society

RESOURCES