Activation of ATP-sensitive potassium channels antagonize nociceptive behavior and hyperexcitability of DRG neurons from rats

作者：Du, Xiaona; Wang, Chao; Zhang, Hailin

来源：Molecular Pain, 2011, 7: 35.

DOI：10.1186/1744-8069-7-35

• K-ATP potassium channels
• DRG
• excitability
• nociception
• pinacidil
• diazoxide
• glyburide

Background: Nociceptive responses to noxious stimuli are initiated at peripheral nociceptor terminals. Ion channels play a vital role in pain signal initiation and conduction. Activation of K-ATP channels has been implicated in mediating the analgesic effects of agents such as morphine. However, systematic studies regarding the effects of K-ATP activators on nociception and neuronal excitability are scarce.
Results: In this study, we describe the antagonistic effects of K-ATP activators pinacidil and diazoxide on nocifensive behavior induced by bradykinin (BK), thermo and mechanical stimuli, and the bradykinin-induced hyperexcitability of DRG neurons. We also found that K-ATP activators can moderately activate K-ATP in DRG neurons. Because the effects of K-ATP activators can be reversed by the K-ATP blocker glyburide, direct activation of K-ATP is most likely the underlying mechanism.
Conclusion: This systematic study clearly demonstrates that activation of K-ATP could have significant modulatory effects on the excitability of sensory neurons and thus on sensory behaviors, such as nociception. K-ATP activators can be evaluated clinically for the treatment of pain symptoms.

• 出版日期2011-5-14
• 单位河北医科大学