کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1366155 | 981582 | 2006 | 16 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors
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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 of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors](/preview/png/1366155.png)
چکیده انگلیسی
In an effort to improve diazabicycloalkane-based opioid receptor ligands, N-3(6)-arylpropenyl-N-6(3)-propionyl-3,6-diazabicyclo[3.1.1]heptanes (3A,Ba–i) were synthesized and their affinity and selectivity towards μ-, δ- and κ-receptors were evaluated.The results of the current study revealed a number of compounds (3Bb, 3Bg and 3Bh) having a high affinity for μ (Ki at μ-receptors ranging from 2.7 to 7.9 nM) versus δ (Ki at δ-receptors >2000 nM) and versus κ (Ki at κ-receptors >5000 nM) receptors.Molecular modelling carried out on the pair 3Aa/3Ba and on the 3Bh was consistent with the hypothesis that the two series of compounds 3A and 3B interact with the μ-receptor in very different ways.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 3, 1 February 2006, Pages 676–691
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 3, 1 February 2006, Pages 676–691
نویسندگان
Giovanni Loriga, Ilaria Manca, Gabriele Murineddu, Giorgio Chelucci, Stefania Villa, Stefania Gessi, Lucio Toma, Giorgio Cignarella, Gerard A. Pinna,