کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358741 | 981359 | 2015 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of orally-bioavailable antagonists of the TRPV4 ion-channel
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Antagonists of the TRPV4 receptor were identified using a focused screen, followed by a limited optimization program. The leading compounds obtained from this exercise, RN-1665 23 and RN-9893 26, showed moderate oral bioavailability when dosed to rats. The lead molecule, RN-9893 26, inhibited human, rat and murine variants of TRPV4, and showed excellent selectivity over related TRP receptors, such as TRPV1, TRPV3 and TRPM8. The overall profile for RN-9893 may permit its use as a proof-of-concept probe for in vivo applications.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 4011–4015
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 4011–4015
نویسندگان
Zhi-Liang Wei, Margaret T. Nguyen, Donogh J.R. O’Mahony, Alejandra Acevedo, Sheila Zipfel, Qingling Zhang, Luna Liu, Michelle Dourado, Candace Chi, Victor Yip, Jeff DeFalco, Amy Gustafson, Daniel E. Emerling, Michael G. Kelly, John Kincaid,