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UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist.

UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist. Following i.v. administration of UK-240455 to male rats, UK-240455 has a clearance of 12 mL/min/kg and a volume of distribution of 0.4 L/kg. The plasma concentration of UK-240455 decreases with an apparent half-life of 0.4 h. Analysis of urine (0 to 24 h) for unchanged UK-240455 indicates that 57% of the dose administered is excreted unchanged in the urine. The urinary clearance of UK-240455 in the rat is therefore 7 mL/min/kg. Following oral administration of UK-240455 to male rats, the apparent elimination half-life of UK-240455 from plasma following oral administration is 1.6 h[1].

[1]. Webster R, et al. Pharmacokinetics and disposition of a novel NMDA glycine site antagonist (UK-240,455) in rats, dogs and man. Xenobiotica. 2003 May;33(5):541-60.

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