کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371312 | 981842 | 2015 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Small molecule (1) has been identified as a selective partial agonist of Opioid Receptor Like-1 (ORL-1) with potential utility for the treatment of anxiety and other disorders. Nociceptin (orphanin FQ) is an endogenous peptide ligand that binds to ORL-1, however it does not bind the classical δ, μ and κ opioid receptors with high affinity. The synthesis of 1 involved using a molecular diversity approach, to rapidly advance a library of compounds for biological testing. A lead selective potent partial agonist (35-fold ORL-1/Mu) progressed to ORL-1 (NOP or OP4) proof of concept testing in advanced studies. The synthetic approach and biological data for the related chemical series will be presented.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 3, 1 February 2015, Pages 602–606
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 3, 1 February 2015, Pages 602–606
نویسندگان
Tina Morgan Ross, Kathleen Battista, Gilles C. Bignan, Doug E. Brenneman, Peter J. Connolly, Jingchun Liu, Steven A. Middleton, Michael Orsini, Allen B. Reitz, Dan I. Rosenthal, Malcolm K. Scott, Anil H. Vaidya,