کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375987 | 981948 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2) Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)](/preview/png/1375987.png)
چکیده انگلیسی
Salvinorin A is the only known non-nitrogenous and specific κ-opioid agonist. A series of salvinorin A derivatives were prepared and tested for in vitro activity at the κ-opioid receptor. Unsubstituted carbamate 9 was a potent κ-agonist (EC50 = 6.2 nM) and should be more stable than salvinorin A toward metabolic transformations. Compound 10, containing an N-methyl carbamate at C(2), showed partial agonist activity with 81% efficacy when compared with the full agonist U50,488H. No antagonist ligands were observed.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 11, 2 June 2005, Pages 2761–2765
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 11, 2 June 2005, Pages 2761–2765
نویسندگان
Cécile Béguin, Michele R. Richards, Yulin Wang, Yong Chen, Lee-Yuan Liu-Chen, Zhongze Ma, David Y.W. Lee, William A. Carlezon Jr., Bruce M. Cohen,