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Effects of clonidine on the activity of the rat glutamate transporter EAAT3 expressed in Xenopus oocytes

Effects of clonidine on the activity of the rat glutamate transporter EAAT3 expressed in Xenopus oocytes
Woo J.H.Han J.I.Baik H.J.Lee H.
Ewha Authors
한종인scopus; 백희정scopus; 이희승scopus; 우재희scopus
Issue Date
Journal Title
Korean Journal of Anesthesiology
2005-6419JCR Link
vol. 62, no. 3, pp. 266 - 271
SCOPUS; KCI scopus
Background: Clonidine has been shown to be a potent neuroprotectant by acting at α 2 receptors on glutamatergicneurons to inhibit the release of glutamate. The aim of this study is to investigate the effects of clonidine on theactivity of EAAT3 that can regulate extracellular glutamate.Methods: EAAT3 was expressed in the Xenopus oocytes. Using a two-electrode voltage clamp, membrane currentswere recorded after application of 30 μM L-glutamate both in the presence and absence of various concentrationsof clonidine. To determine the effects of clonidine on the K m and Vmax of EAAT3 and the reversibility of clonidineeffects, membrane currents were recorded after the application of various concentrations of L-glutamate both in thepresence and absence of 1.50 × 10 -7 M clonidine. Results: Clonidine reduced the EAAT3 responses to L-glutamate in a concentration-dependent manner. Thisinhibition was statistically significant at higher concentrations than at the clinically relevant range. Clonidine at 1.50× 10 -7 M reduced the Vmax, but did not affect the K m of EAAT3 for L-glutamate.Conclusions: These results suggest that the direct inhibition of EAAT3 activity is not related to the sedation effectof clonidine and that the clonidine-induced reduction of EAAT3 activity provides additional data for the possibleinvolvement of glutamatergic hyperactivity in the proconvulsant effect of clonidine. © the Korean Society of Anesthesiologists, 2012.
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