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Scheibler P, Kronfeld A, Illes P, Allgaier C: Trichloroethanol impairs NMDA receptor function in rat mesencephalic and cortical neurones. Eur J Pharmacol. 1999 Feb 5;366(2-3):R1-2. 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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