Add time:08/24/2019 Source:sciencedirect.com
The effects of 2,2,2-trichloroethanol, the active compound of the sedative–hypnotic chloral hydrate, were investigated on N-methyl-d-aspartate (NMDA)-induced increases in intracellular Ca2+ concentration ([Ca2+]i) in cultured mesencephalic and cortical neurones by means of the fura-2 method. Trichloroethanol inhibited the NMDA response in a concentration-dependent manner in cortical (IC50=2.76 mM) and mesencephalic neurones (IC50=1.12 mM), with a maximum effect of approximately 85 and 94%, respectively. Ethanol was considerably less potent than trichloroethanol. In conclusion, the trichloroethanol-induced impairment of NMDA receptor function may contribute to the sedative–hypnotic properties of chloral hydrate.
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