[Modulation of SKF38393 and clonidine on expressed GABA(A) receptors in Xenopus oocytes]

Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2001 Nov;17(4):333-6.
[Article in Chinese]

Abstract

Aim and methods: The present research is performed on Xenopus oocytes injected with rat DRG mRNA. Modulatory effects of SKF38393 and Clonidine on GABAS(A) receptors expressed in Xenopus oocytes was investigated by two-electrodes voltage-clamp technique, and it is compared with the neurons fresh isolated.

Results: It is found that SKF38393 and Clonidine inhibitable GABA(A) receptor function obviously by a concentration-dependent manner. There is an interaction between SKF38393- and Clonidine-induced currents. The inhibition of SKF38393 and Clonidine on GABA(A) receptors is noncompetitive and voltage-independent.

Conclusions: The results suggest that the inhibition by SKF38393 and clonidine of GABA-activated current might be a result of phosphorylation of GABA(A) receptor following action of second messenger and the thereby mediated intracellular transduction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine / pharmacology*
  • Animals
  • Clonidine / pharmacology*
  • Female
  • Neurons / drug effects
  • Neurons / metabolism
  • Oocytes / drug effects*
  • Oocytes / metabolism*
  • Phosphorylation
  • RNA, Messenger
  • Rats
  • Rats, Wistar
  • Receptors, GABA-A / metabolism*
  • Second Messenger Systems
  • Xenopus

Substances

  • RNA, Messenger
  • Receptors, GABA-A
  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
  • Clonidine