Azulene as a biphenyl mimetic in orexin/hypocretin receptor agonists
Leino, T. O., Turku, A., Urvas, L., Adhikari, K., Oksanen, J., Steynen, Y., Yli-Kauhaluoma, J., Xhaard, H., Kukkonen, J. P., & Wallén, E. A.A. (2023). Azulene as a biphenyl mimetic in orexin/hypocretin receptor agonists. Bioorganic and Medicinal Chemistry, 88-89, Article 117325. https://doi.org/10.1016/j.bmc.2023.117325
Julkaistu sarjassa
Bioorganic and Medicinal ChemistryPäivämäärä
2023Tekijänoikeudet
© 2023 The Author(s). Published by Elsevier Ltd.
Azulene is a rare ring structure in drugs, and we investigated whether it could be used as a biphenyl mimetic in known orexin receptor agonist Nag 26, which is binding to both orexin receptors OX1 and OX2 with preference towards OX2. The most potent azulene-based compound was identified as an OX1 orexin receptor agonist (pEC50 = 5.79 ± 0.07, maximum response = 81 ± 8% (s.e.m. of five independent experiments) of the maximum response to orexin-A in Ca2+ elevation assay). However, the azulene ring and the biphenyl scaffold are not identical in their spatial shape and electron distribution, and their derivatives may adopt different binding modes in the binding site.
Julkaisija
Elsevier BVISSN Hae Julkaisufoorumista
0968-0896Julkaisu tutkimustietojärjestelmässä
https://converis.jyu.fi/converis/portal/detail/Publication/183153867
Metadata
Näytä kaikki kuvailutiedotKokoelmat
Rahoittaja(t)
Suomen AkatemiaRahoitusohjelmat(t)
Tutkijatohtori, SALisätietoja rahoituksesta
T.O.L. acknowledges the Doctoral Program in Drug Research of the University of Helsinki and the Academy of Finland (grant no. 330800); A.T. acknowledges the Finnish Cultural Foundation and the Orion Research Foundation; and J.P.K. acknowledges the Magnus Ehrnrooth Foundation, the Liv & Hälsa Foundation and Finska läkaresällskapet for financial support. Marja Peltola, Santeri Suokas and Maiju K. R ...
Lisenssi
Ellei muuten mainita, aineiston lisenssi on CC BY 4.0