Inhibition by bis(7)-tacrine of 5-HT-activated current in rat TG neurons

Jia Lie Luo, Jian Zhang, Bing Cai Guan, Yuan Ping Pang, Yi Fan Han, Zhi Wang Li

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

Whole-cell recordings were performed on rat trigeminal ganglion (TG) neurons as a modeling experiment to investigate the effect of bis (7)-tacrine, a potential anti-Alzheimer's disease (AD) drug, on 5-HT-induced current (I 5-HT). Extracellular 5-HT activated a concentration-dependent inward current that was blocked by ICS 205930. Co-application of bis(7)-tacrine inhibited I5-HT markedly with IC50 at 2 × 10 -6 M. Bis(7)-tacrine shifted the concentration-response curve for I5-HT rightwards with its maximum response unchanged and EC 50 increased, suggesting that this inhibition was competitive in nature. Intracellular dialysis of GDP-β-S did not block bis(7)-tacrine inhibition of I5-HT, which excluded the involvement of G-protein mediation. These results may offer possible modality to understanding the anti-AD mechanism of bis(7)-tacrine.

Original languageEnglish (US)
Pages (from-to)1335-1338
Number of pages4
JournalNeuroReport
Volume15
Issue number8
DOIs
StatePublished - Jun 7 2004

Keywords

  • 5-HT receptor
  • Bis(7)-tacrine
  • Current
  • Inhibition
  • Rat
  • Trigeminal ganglion

ASJC Scopus subject areas

  • Neuroscience(all)

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