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; Yifan Han; Zhi Wang Li

doi:10.1097/01.wnr.0000127075.51445.3e

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, Yifan Han, Zhi Wang Li

Research output: Journal article publication › Journal article › Academic research › peer-review

7 Citations (Scopus)

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 (I5-HT). Extracellular 5-HT activated a concentration-dependent inward current that was blocked by ICS 205930. Co-application of bis(7)-tacrine inhibited I5-HTmarkedly with IC50at 2 × 10-6M. Bis(7)-tacrine shifted the concentration-response curve for I5-HTrightwards with its maximum response unchanged and EC50increased, 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 language	English
Pages (from-to)	1335-1338
Number of pages	4
Journal	NeuroReport
Volume	15
Issue number	8
DOIs	https://doi.org/10.1097/01.wnr.0000127075.51445.3e
Publication status	Published - 7 Jun 2004
Externally published	Yes

Keywords

5-HT receptor 3
Bis(7)-tacrine
Current
Inhibition
Rat
Trigeminal ganglion

ASJC Scopus subject areas

General Neuroscience

More information

10.1097/01.wnr.0000127075.51445.3e

Cite this

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

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 (I5-HT). Extracellular 5-HT activated a concentration-dependent inward current that was blocked by ICS 205930. Co-application of bis(7)-tacrine inhibited I5-HTmarkedly with IC50at 2 × 10-6M. Bis(7)-tacrine shifted the concentration-response curve for I5-HTrightwards with its maximum response unchanged and EC50increased, 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.",

keywords = "5-HT receptor 3, Bis(7)-tacrine, Current, Inhibition, Rat, Trigeminal ganglion",

author = "Luo, {Jia Lie} and Jian Zhang and Guan, {Bing Cai} and Pang, {Yuan Ping} and Yifan Han and Li, {Zhi Wang}",

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AU - Luo, Jia Lie

AU - Zhang, Jian

AU - Guan, Bing Cai

AU - Pang, Yuan Ping

AU - Han, Yifan

AU - Li, Zhi Wang

PY - 2004/6/7

Y1 - 2004/6/7

N2 - 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 (I5-HT). Extracellular 5-HT activated a concentration-dependent inward current that was blocked by ICS 205930. Co-application of bis(7)-tacrine inhibited I5-HTmarkedly with IC50at 2 × 10-6M. Bis(7)-tacrine shifted the concentration-response curve for I5-HTrightwards with its maximum response unchanged and EC50increased, 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.

AB - 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 (I5-HT). Extracellular 5-HT activated a concentration-dependent inward current that was blocked by ICS 205930. Co-application of bis(7)-tacrine inhibited I5-HTmarkedly with IC50at 2 × 10-6M. Bis(7)-tacrine shifted the concentration-response curve for I5-HTrightwards with its maximum response unchanged and EC50increased, 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.

KW - 5-HT receptor 3

KW - Bis(7)-tacrine

KW - Current

KW - Inhibition

KW - Rat

KW - Trigeminal ganglion

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C2 - 15167561

SN - 0959-4965

VL - 15

SP - 1335

EP - 1338

JO - NeuroReport

JF - NeuroReport

IS - 8

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

More information

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