• Anesthesia and analgesia · Jul 2000

    The stereoselective effects of ketamine isomers on heteromeric N-methyl-D-aspartate receptor channels.

    • T Yamakura, K Sakimura, and K Shimoji.
    • Department of Anesthesiology, Niigata University School of Medicine, Japan. yamakura@med.niigata-u.ac.jp
    • Anesth. Analg. 2000 Jul 1; 91 (1): 225-9.

    UnlabelledThe effects of S(+)- and R(-)-ketamine on heteromeric N-methyl-D-aspartate receptor channels were investigated on the epsilon1/zeta1, epsilon2/zeta1, epsilon3/zeta1, and epsilon4/zeta1 channels expressed in Xenopus oocytes. S(+)-ketamine inhibited all four epsilon/zeta channels more effectively than R(-)-ketamine. The inhibitor concentrations for half-control response for S(+)-ketamine were quite similar among the four channels with 0.44-0.56 microM. However, the inhibitor concentrations for half-control response for R(-)-ketamine varied slightly among the four channels with 1.0 microM for epsilon2/zeta1 and epsilon3/zeta1 channels and 1.9-2.0 microM for epsilon1/zeta1 and epsilon4/zeta1 channels. Thus, the potency ratio of S(+)- and R(-)-ketamine for heteromeric channels was only slightly different among the epsilon/zeta channels.ImplicationsThe potency order and ratio of ketamine isomers for inhibition of N-methyl-D-aspartate receptor channels may not be so different between the brain region and the developmental stage.

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