کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5554518 | 1558871 | 2017 | 28 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Mechanistic evaluation of tapentadol in reducing the pain perception using in-vivo brain and spinal cord microdialysis in rats
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Mechanistic evaluation of tapentadol in reducing the pain perception using in-vivo brain and spinal cord microdialysis in rats Mechanistic evaluation of tapentadol in reducing the pain perception using in-vivo brain and spinal cord microdialysis in rats](/preview/png/5554518.png)
چکیده انگلیسی
Role of monoamine neurotransmitters in the modulation of emotional and pain processing in spinal cord and brain regions is not well known. Tapentadol, a norepinephrine reuptake inhibitor with µ-opioid receptor agonistic activity has recently been introduced for the treatment of moderate to severe pain. The objective of the present study was to examine the effects of tapentadol on modulation of monoamines in the prefrontal cortex and dorsal horn using brain microdialysis. Tapentadol was administered intraperitoneally at 4.64-21.5 mg/kg to male Wistar rats. Based on these results, 10 mg/kg i.p. was chosen for spinal microdialysis in freely moving rats. Tapentadol produced significant and dose-dependent increase in cortical dopamine and norepinephrine levels with mean maximum increase of 600% and 300%, respectively. Treatment had no effect on cortical serotonin levels. In the dorsal horn, serotonin, dopamine and norepinephrine levels were significantly increased with mean maximum increases of 220%, 190% and 280%, respectively. Although the density of dopamine transporter is low in cortex, the increase of dopamine and norepinephrine levels in cortex could be mediated through the inhibition of norepinephrine transporter. In the dorsal horn, increase in norepinephrine levels could be due to inhibition of norepinephrine transporter in the spinal cord. Whereas, activation of opioids receptors in non-spinal regions might be responsible for increase in dopamine and serotonin levels. The results from current investigation suggest that clinical efficacy of tapentadol in neuropathic pain is mediated through the enhanced monoaminergic neurotransmission in the spinal cord and regions involved with emotional processing in brain.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 809, 15 August 2017, Pages 224-230
Journal: European Journal of Pharmacology - Volume 809, 15 August 2017, Pages 224-230
نویسندگان
Vijay Benade, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Saivishal Daripelli, Ganesh Ayyanki, Shantaveer Irappanavar, Ranjithkumar Ponnamaneni, Arunkumar Manoharan,