دورية أكاديمية
Azulene-based compounds for targeting orexin receptors
| العنوان: | Azulene-based compounds for targeting orexin receptors |
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| المؤلفون: | Leino, Teppo O., Turku, Ainoleena, Yli-Kauhaluoma, Jari Tapani, Kukkonen, Jyrki P., Xhaard, Henri, Wallén, Erik A. A. |
| المساهمون: | Faculty of Pharmacy, Pharmaceutical Design and Discovery group, Division of Pharmaceutical Chemistry and Technology, Drug Research Program, Jari Yli-Kauhaluoma / Principal Investigator, Jyrki Kukkonen / Principal Investigator, Veterinary Biochemistry and Cell Biology, Veterinary Biosciences, Departments of Faculty of Veterinary Medicine, Faculty of Veterinary Medicine, Department of Physiology, Medicum, Henri Xhaard / Principal Investigator, Erik Wallen / Principal Investigator, Medicinal Chemistry research group |
| بيانات النشر: | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| سنة النشر: | 2020 |
| المجموعة: | Helsingfors Universitet: HELDA – Helsingin yliopiston digitaalinen arkisto |
| مصطلحات موضوعية: | 317 Pharmacy, 116 Chemical sciences, Azulene, Orexin receptor, Potentiator, Agonist, Antagonist, Sleep-wake regulation, PROTEIN-COUPLED RECEPTORS, HAMSTER OVARY CELLS, SIGNAL-TRANSDUCTION, CA2+ INFLUX, OX1, DERIVATIVES, INHIBITORS, PEPTIDES, LIGANDS, KINASE |
| الوصف: | A library of 70 000 synthetically accessible azulene-based compounds was virtually screened at the OX2 receptor. Based on the results, a series of azulene derivatives was synthesized and the binding to and activation of both orexin receptor subtypes were assessed. Two most promising binders were determined to have inhibition constants in the 3-9 mu M range and two other compounds showed weak OX2 receptor agonism. Furthermore, three compounds exhibited a concentration-dependent potentiation of the response to orexin-A at the OX1 but not the OX2 receptors. Altogether this data opens new approaches for further development of antagonists, agonists, and potentiators of orexin response based on the azulene scaffold. (C) 2018 Elsevier Masson SAS. All rights reserved. ; Peer reviewed |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| ردمك: | 978-85-05-08493-0 85-05-08493-4 |
| العلاقة: | Leino , T O , Turku , A , Yli-Kauhaluoma , J T , Kukkonen , J P , Xhaard , H & Wallén , E A A 2018 , ' Azulene-based compounds for targeting orexin receptors ' , European Journal of Medicinal Chemistry , vol. 157 , pp. 88-100 . https://doi.org/10.1016/j.ejmech.2018.07.040Test; ORCID: /0000-0003-0370-7653/work/50286680; ORCID: /0000-0003-0959-7221/work/50289879; ORCID: /0000-0003-2582-7971/work/50290708; ORCID: /0000-0002-6989-1564/work/63349244; http://hdl.handle.net/10138/319069Test; be64b9c4-f27c-4b99-9902-88569234386b; 85050849346; 000447480000008 |
| الإتاحة: | http://hdl.handle.net/10138/319069Test |
| حقوق: | cc_by_nc_nd ; info:eu-repo/semantics/openAccess ; openAccess |
| رقم الانضمام: | edsbas.8392A61B |
| قاعدة البيانات: | BASE |
| ردمك: | 9788505084930 8505084934 |
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