Add time:08/31/2019         Source:sciencedirect.com

The effects of chloral hydrate and its main metabolite 2,2,2-Trichloroethanol (cas 115-20-8) were investigated on the (S)-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA)-induced rise of intracellular Ca2+ concentration ([Ca2+]i) in cultured non-pyramidal cortical neurones of rats by using single-cell fura-2 microfluorimetry. AMPA elicited a concentration-dependent effect that peaked at 300 μM (EC50, 7.5 μM). Responses to AMPA (30 μM) were markedly inhibited by superfusion with chloral hydrate (IC50, 4.5 mM) or trichloroethanol (IC50, 0.9 mM). By contrast, ethanol (100 mM) caused only slight inhibition. In conclusion, the results demonstrate that chloral hydrate and especially its metabolite trichloroethanol, inhibit the AMPA-induced rise of [Ca2+]i by depressing the entry of Ca2 into cortical neurones via the AMPA receptor-channel.

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