کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9921442 | 1559221 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Role of 5-HT1A and 5-HT1B receptors in the antinociceptive effect of tramadol
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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: Role of 5-HT1A and 5-HT1B receptors in the antinociceptive effect of tramadol Role of 5-HT1A and 5-HT1B receptors in the antinociceptive effect of tramadol](/preview/png/9921442.png)
چکیده انگلیسی
Tramadol, (1RS,2RS)-2-[(dimethylamine)-methyl]-1-(3-methoxyphenyl)-cyclohexanol hydrochloride, is an atypical centrally acting analgesic agent with relatively weak opioid receptor affinity and which, like some antidepressants, is able to inhibit the reuptake of serotonin (5-hydroxytryptamine, 5-HT) in the raphe nucleus. We have previously demonstrated that pindolol, a beta-adrenoceptor blocker/5-hydroxytryptamine1A/1B receptor antagonist, enhanced tramadol antinociception and that the selective 5-HT1A agonist 8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) reduced it. These effects were related to the negative feedback control that regulates raphe region neurones. The current study examines the ability of the selective antagonist at somatodendritic 5-HT1A receptors, N-{2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl}-N-(2-pyridinyl) cyclohexane carboxamide (WAY100635, 0.8 mg/kg), the selective antagonist at terminal 5-HT1B receptors, N-[3-(2-dimethylamino) ethoxy-4-methoxyphenyl]-2â²-methyl-4â²-(5-methyl-1,2,4-oxadiazol-3-yl)-(1,1â²-biphenyl)-4-carboxamide (SB216641, 0.1-0.8 mg/kg) and the selective agonist at 5-HT1B receptors, 1,4-tDihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrolo[3,2-b] pyridin-5-one (CP93129, 0.2-0.4 mg/kg), to modify the antinociceptive effect of 4-64 mg/kg of tramadol in the hot plate test in mice. The results show that 0.8 mg/kg of WAY100635 enhanced antinociceptive effect of tramadol while neither agonism nor antagonism at the 5-HT1B receptor modifies it significantly at the doses tested. These results account for involvement of the somatodendritic 5-HT1A receptors in the analgesic effect of tramadol and support the supraspinal interaction of serotonin and the opioid system in the regulation of pain.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 511, Issue 1, 21 March 2005, Pages 21-26
Journal: European Journal of Pharmacology - Volume 511, Issue 1, 21 March 2005, Pages 21-26
نویسندگان
M. Olga Rojas-Corrales, Esther Berrocoso, Juan A. Micó,