The tyrosine kinase inhibitor genistein directly inhibits GABA(A) receptors

Ren Qi Huang, Ming Jun Fang, Glenn H. Dillon

Research output: Contribution to journalArticle

50 Citations (Scopus)

Abstract

The protein tyrosine kinase (PTK) inhibitor genistein has been widely used to examine potential effects of tyrosine phosphorylation on neurotransmitter function. We report here that genistein inhibits GABA(A) receptors through a direct effect. Extracellular application of genistein and GABA reversibly inhibited GABA-activated currents recorded from HEK293 cells expressing rat α1β2γ2S or α1β2 receptors, even when genistein was preequilibrated in the intracellular solution. Daidzein, an analog of genistein that does not block PTK, also inhibited GABA-activated current. Coapplication of lavendustin A, a specific inhibitor of PTK, had no effect on the GABA response. Our results demonstrate that genistein has a direct inhibitory effect on GABA(A) receptors that is not mediated via inhibition of tyrosine kinase.

Original languageEnglish
Pages (from-to)177-183
Number of pages7
JournalMolecular Brain Research
Volume67
Issue number1
DOIs
StatePublished - 6 Apr 1999

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Genistein
GABA-A Receptors
Protein-Tyrosine Kinases
gamma-Aminobutyric Acid
HEK293 Cells
Protein Kinase Inhibitors
Neurotransmitter Agents
Tyrosine
Phosphorylation

Keywords

  • Daidzein
  • Genistein
  • Lavendustin A
  • Protein tyrosine phosphorylation
  • Recombinant GABA(A) receptor
  • Tyrosine kinase

Cite this

Huang, Ren Qi ; Fang, Ming Jun ; Dillon, Glenn H. / The tyrosine kinase inhibitor genistein directly inhibits GABA(A) receptors. In: Molecular Brain Research. 1999 ; Vol. 67, No. 1. pp. 177-183.
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The tyrosine kinase inhibitor genistein directly inhibits GABA(A) receptors. / Huang, Ren Qi; Fang, Ming Jun; Dillon, Glenn H.

In: Molecular Brain Research, Vol. 67, No. 1, 06.04.1999, p. 177-183.

Research output: Contribution to journalArticle

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