کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9921589 | 1559228 | 2005 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Actions of tilidine and nortilidine on cloned opioid receptors
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
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چکیده انگلیسی
Tilidine, alone or combined with naloxone to prevent drug abuse, is used as an oral opioid analgesic. Although the analgesic action of tilidine and its active metabolite nortilidine is reversed by naloxone and therefore believed to involve the activation of the Mu opioid (MOP, OP3, μ) receptor, this has never been studied in recombinant systems. We have measured the selectivity of tilidine and nortilidine for human opioid and opioid-like receptors stably expressed in CHO-K1 cells, using the inhibition of the forskolin (FK)-induced accumulation of cAMP as endpoint. In cells expressing the MOP receptor, tilidine and nortilidine inhibited cAMP accumulation with IC50 of 11 μM and 110 nM, respectively. The agonist effects of nortilidine and [d-Ala2-MePhe4-Gly5-ol]enkephalin (DAMGO) on the MOP receptor were reversed by naloxone with very similar IC50 (1.2 versus 1.8 nM). At concentrations up to 100 μM, tilidine and nortilidine had no agonist effect on the DOP, KOP and NOP receptors. In conclusion, this study on cloned human receptors demonstrates that nortilidine is a selective agonist of the MOP receptor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 506, Issue 3, 4 January 2005, Pages 205-208
Journal: European Journal of Pharmacology - Volume 506, Issue 3, 4 January 2005, Pages 205-208
نویسندگان
Christophe Thierry, Jean-Marie Boeynaems, Meoni Paolo,