Nisoxetine produces local but not systemic analgesia against cutaneous nociceptive stimuli in the rat

作者：Chen Yu Wen; Chu Chin Chen; Chen Yu Chung; Wang Jhi Joung; Hung Ching Hsia^*; Shao Dong Zi

来源：European Journal of Pharmacology, 2012, 675(1-3): 22-25.

DOI：10.1016/j.ejphar.2011.11.042

• Nisoxetine
• MK-801
• Lidocaine
• Additive effect
• Cutaneous anesthesia

The aim of this study was to evaluate the local anesthetic effect of nisoxetine as infiltrative cutaneous analgesic. After rats were injected subcutaneously with nisoxetine, dose-response curves were constructed. The cutaneous anesthetic effect of nisoxetine or MK-801 (dizocilpine) was compared with lidocaine, a traditional local anesthetic. We found that nisoxetine and MK-801 acted like lidocaine and elicited dose-related cutaneous (local) anesthesia. The relative potency was nisoxetine %26gt; MK-801 %26gt; lidocaine (P%26lt;0.01) as infiltrative anesthesia of skin. On an equianesthetic doses (20% effective dose [ED20], ED50, and ED80), nisoxetine produced longer action of cutaneous anesthesia than that of lidocaine or MK-801 (P%26lt;0.01). Coadministration of nisoxetine or lidocaine with MK-801 showed an additive cutaneous anesthesia. Neither local injection of a large dose of nisoxetine, MK-801 nor lidocaine in the thigh area produced cutaneous anesthesia (data not shown). In conclusion, nisoxetine had a local anesthetic effect as infiltrative cutaneous analgesia with durations of actions longer than that of lidocaine or MK-801. That N-methyl-D-aspartate receptors may not contribute to the cutaneous (local) anesthetic effect of nisoxetine or lidocaine.

• 出版日期2012-1-30
• 单位中国医科大学