Summary
The effect of exogenous choline on the outflow of 3H-acetylcholine evoked by field stimulation was studied on the myenteric plexus-longitudinal muscle preparation of the guinea pig. Choline at concentrations of 100 μM and higher depressed the evoked outflow of 3H-acetylcholine in a concentration-dependent manner. The EC 50 for the inhibitory action was 300 μM. Scopolamine (10 nM) antagonized the effect of choline which indicates that the inhibition of 3H-acetylcholine outflow is mediated by muscarine receptors. The findings imply that choline at high concentrations does not improve cholinergic synaptic neurotransmission in tissues that are endowed with presynaptic muscarine receptors (e.g. myenteric and central cholinergic neurones). Furthermore, it is suggested that the increase in tissue acetylcholine content that has been observed after choline administration is probably due to the depression of acetylcholine release.
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References
Cohen EL, Wurtman RJ (1975) Brain acetylcholine: increase after systemic choline administration. Life Sci 16:1095–1102
Consolo S, Ladinsky H, Gomeni R (1979) Effect of high plasma choline on brain area acetylcholine content: durg intervention. Pharmacol Res Commun 11:903–919
Davis KL, Berger PA, Hollister LE (1979) Clinical and preclinical experience with choline chloride in Huntington's disease and tardive dyskinesia: Unanswered questions. In: Barbeau A, Growdon JH, Wurtman RJ (eds) Nutrition of the brain: Choline and lecithin in brain disorders, vol 5. Raven Press, New York, pp 305–315
Dieterich HA, Lindmar R, Löffelholz K (1978) The role of choline in the release of acetylcholine in isolated hearts. Naunyn-Schmiedeberg's Arch Pharmacol 301:207–215
Eckernäs SA, Sahlström L, Aquilonius SM (1977) In vivo turnover rate of acetylcholine in rat brain parts at elevated steady-state concentration of plasma choline. Acta Physiol Scand 101:404–410
Fosbraey P, Johnson ES (1980) Modulation by acetylcholine of the electrically-evoked release of 3H-acetylcholine from the ileum of the guinea-pig. Br J Pharmacol 69:145–149
Haubrich DR, Wedeking PW, Wang PFL (1974) Increase in tissue concentration of acetylcholine in guinea pigs in vivo induced by administration of choline. Life Sci 14:921–927
Haubrich DR, Wang PFL, Clody DE, Wedeking PW (1975) Increase in rat brain acetylcholine induced by choline or deanol. Life Sci 17:975–980
Hrdina PD (1974) Metabolism of brain acetylcholine and its modification by drugs. Drug Metabol Rev 3:89–129
Kilbinger H, Wagner P (1975) Inhibition by oxotremorine of acetylcholine resting release from guinea-pig ileum longitudinal muscle strips. Naunyn-Schmiedeberg's Arch Pharmacol 287:47–60
Kilbinger H, Wessler I (1980a) Inhibition by acetylcholine of the stimulation-evoked release of 3H-acetylcholine from the guinea-pig myenteric plexus. Neuroscience 5:1331–1340
Kilbinger H, Wessler I (1980b) Pre- and postsynaptic effects of muscarinic agonists in the guinea-pig ileum. Naunyn-Schmiedeberg's Arch Pharmacol 314:259–266
Kilbinger H, Kruel R, Wessler I (1980) Modulation by scopolamine, acetylcholine and choline of the evoked release of acetylcholine from guinea-pig myenteric plexus: Evidence for a muscarinic feedback inhibition of acetylcholine secretion. Symp on Cholin. Mechanisms, Florence, March 1980. Plenum Press New York (in press)
Kosterlitz HW, Lydon RJ, Watt AJ (1970) The effects of adrenaline, noradrenaline and isoprenaline on inhibitory α- and β-adrenoceptors in the longitudinal muscle of the guinea-pig ileum. Br J Pharmacol 39:398–413
Krnjević K, Reinhardt W (1979) Choline excites cortical neurons. Science 206:1321–1323
MacIntosh FC (1979) Are acetylcholine levels related to acetylcholine release? In: Barbeau A, Growdon JH, Wurtman RJ (eds) Nutrition and the brain: Choline and lecithin in brain disorders, vol 5. Raven Press, New York, pp 201–217
MacIntosh FC, Collier B (1976) Neurochemistry of cholinergic terminals. In: Zaimis E (ed) Handbuch der exp. Pharmakologie, vol 42. Springer, Berlin Heidelberg New York, pp 99–228
Pepeu G (1973) The release of acetylcholine from the brain: An approach to the study of the central cholinergic mechanisms. Progr Neurobiol 2:257–288
Pomeroy AR, Raper C (1972) Cholinomimetic activity of dimethylamino-ethanol, and-propanol and related compounds. Eur J. Pharmac 17:81–86
Szerb J (1976) Storage and release of labelled acetylcholine in the myenteric plexus of the guinea-pig ileum. Can J Physiol Pharmacol 54:12–22
Szerb JC (1979) Autoregulation of acetylcholine release. In: Langer SZ, Starke K, Dubocovich ML (eds) Presynaptic receptors. Pergamon Press, Oxford, pp 293–298
Ulus IH, Arslan Y, Tanrisever R, Kiran BK (1979) Postsynaptic effects of choline administration. In: Barbeau A, Growdon JH, Wurtman RJ (eds) Nutrition and the brain: Choline and lecithin in brain disorders, vol 5. Raven Press, New York, pp 219–225
Wurtman RJ (1979). Precursor control of transmitter synthesis. In: Barbeau A, Growdon JH, Wurtman RJ (eds) Nutrition and the brain: Choline and lecithin in brain disorders, vol 5. Raven Press, New York, pp 1–12
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Kilbinger, H., Kruel, R. Choline inhibits acetylcholine release via presynaptic muscarine receptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 316, 131–134 (1981). https://doi.org/10.1007/BF00505306
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DOI: https://doi.org/10.1007/BF00505306