کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361400 | 981462 | 2007 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Fatty acyl amides of endogenous tetrahydroisoquinolines are active at the recombinant human TRPV1 receptor
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Fatty acyl amides of endogenous tetrahydroisoquinolines are active at the recombinant human TRPV1 receptor Fatty acyl amides of endogenous tetrahydroisoquinolines are active at the recombinant human TRPV1 receptor](/preview/png/1361400.png)
چکیده انگلیسی
The SAR of capsazepine revealed that tetrahydroisoquinoline (TIQ) moiety is a core pharmacophore of TRPV1 activity. This implied that conjugates of endogenous TIQs with fatty acids would be active at TRPV1 receptors. Six such compounds were synthesized and tested for calcium mobilization at recombinant TRPV1 receptors overexpressed in HEK293 cells. Three compounds showed partial TRPV1 agonism with EC50 values in the low micromolar range and maximal efficacies between 25% and 55% of capsaicin.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 18, 15 September 2007, Pages 6164–6169
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 18, 15 September 2007, Pages 6164–6169
نویسندگان
David K. O’Dell, Neta Rimmerman, Sarah R. Pickens, J. Michael Walker,