Increasing effect of ethanol on 5-HT3 receptor-mediated 14C-guanidinium influx in N1E-115 neuroblastoma cells
Naunyn-Schmiedebergs Archiv für Pharmakologie und experimentelle Pathologie - Tập 352 Số 2 - Trang 149-156 - 1995
Tóm tắt
NlE-115 mouse neuroblastoma cells were used to study the influence of ethanol on the 5-HT- and veratridine-induced influx of 14C-guanidinium via the 5-HT3 receptor channel and the fast sodium channel, respectively. Ethanol (10–100 mM) concentration-dependently increased the 5-HT-induced 14C-guanidinium influx, leaving the basal and veratridine (100 μM)-induced influx unaffected. The increasing effect of ethanol (100 mM) was observed at all 5-HT concentrations investigated; accordingly, ethanol increased the maximum response to 5-HT. Whereas in the absence of ethanol the concentration-response curve for 5-HT was bell-shaped, this was no longer the case when ethanol (100 mM) was present in the incubation buffer; the descending branch of the concentration-response curve for 5-HT at concentrations above 300 μM was virtually no longer observed. When, in the presence of substance P 10 μM the 5-HT-induced 14C-guanidinium influx was already enhanced, the ability of ethanol (100 mM) to increase the 5-HT-induced influx was considerably diminished (by 72%). Preincubation of N1E-155 cells with 5-HT caused a decay of the subsequent 5-HT response (“desensitization”) which was dependent on the duration of preincubation; ethanol (100 mM) did not affect the rate of this decay of the 5-HT response. The 5-HT (30μM)-induced 14C-guanidinium influx was also increased by methanol (100 mM) and n-propanol (100 mM). The rank order of the increasing effect of the n-alkanols (at 100 mM) was: methanol < ethanol < n-propanol; i.e. the degree of enhancement increased with the lipophilicity of the alcohols. Ethanol (100 mM) did not alter the time-course of non-specific and specific binding of the selective 5-HT3 receptor antagonist 3H-GR 65630 to intact N1E-155 cells. In competition binding experiments, inhibition of 3H-GR 65630 binding by 5-HT was characterized by a high affinity (pIC50 = 4.71 ± 0.19) and a low affinity component (pIC50 = 2.65 ± 0.03). Ethanol did not affect the 5-HT-induced inhibition of 3H-GR 65630 binding. These results indicate that ethanol does not interfere with the 5-HT recognition site of the 5-HT3 receptor. Since the enhancement of cation influx by alcohols increased in proportion to their lipophilicity, it is suggested that ethanol and other n-alkanols interact with a hydrophobic region of the 5-HT3 receptor channel. In analogy to its effect on the nicotinic receptor channel, ethanol may stabilize the open state of the 5-HT3 receptor channel.
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