Strychnine-sensitive glycine receptors inducing [3H]-acetylcholine release in rat caudatoputamen: a new site of action of ethanol? (original) (raw)

Abstract

In the present study acute effects of ethanol on [3H]-acetylcholine ([3H]-ACh) release induced by activation of strychnine-sensitive glycine receptors in superfused slices of rat caudatoputamen were investigated. The glycine-evoked [3H]-ACh release (lg EC50 = –4.10, CI95 = [–4.14, –4.05]) was inhibited by strychnine in a competitive manner (pA2 = 6.86, CI95 = [6.61, 7.08]). Release of [3H]-ACh could also be induced by L-serine. L-serine was less potent than glycine (lg EC50 = –2.61, CI95 = [–2.69, –2.52]). Both glycine and L-serine showed similar maximum effects (Emax(glycine) = 1.34, CI95 = [1.24, 1.45]; Emax(L-serine) = 1.19, CI95 = [1.09, 1.32]). Ethanol at concentrations of 2‰ (= 34 mM) and 4‰ (= 68 mM) inhibited glycine-evoked [3H]-ACh release in a manner like the competitive antagonist strychnine, however with lower potency. The pA2 of ethanol was 1.19, CI95 = [0.85, 1.41], at 2‰ [v/v] and 1.51, CI95 = [1.19, 1.78] at 4‰ ethanol. Similar to its action on glycine-evoked [3H]-ACh release, ethanol at 4‰ [v/v] also inhibited L-serine-evoked transmitter release in a competitive-like fashion (pA2 = 0.83, CI95 = [–0.15, 1.18]). We conclude, that strychnine-sensitive glycine receptors, mediating [3H]-ACh release in the rat caudatoputamen, might represent a new site of action of ethanol.

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Authors and Affiliations

  1. Sektion Klinische Neuropharmakologie der Neurologischen Universitätsklinik, Neurozentrum, Breisacherstrasse 64, D-79106 Freiburg, Germany, , , , , , DE
    M. Darstein, R. Knörle & T. J. Feuerstein
  2. Wyeth-Pharma GmbH, Clinical Research and Development, Schleebrüggenkamp 15, D-48159 Münster, Germany, , , , , , DE
    P. A. Löschmann

Authors

  1. M. Darstein
  2. P. A. Löschmann
  3. R. Knörle
  4. T. J. Feuerstein

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Received: 15 May 1997 / Accepted: 4 September 1997

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Darstein, M., Löschmann, P., Knörle, R. et al. Strychnine-sensitive glycine receptors inducing [3H]-acetylcholine release in rat caudatoputamen: a new site of action of ethanol?.Naunyn-Schmiedeberg's Arch Pharmacol 356, 738–745 (1997). https://doi.org/10.1007/PL00005112

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