5-Hydroxy-2-(2-phenylethyl) chromone (5-HPEC): A novel non-nitrogenous ligand for 5-HT2B receptor

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Williams, Dwight A.¹  Zaidi, Saheem A.²  Zhang, Yan² 

[1] Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA

[2] Virginia Commonwealth Univ, BioTech 1, Dept Med Chem, Richmond, VA 23298 USA

关键词: Chromone;    Neuroprotection;    5-HT2B receptor;    Antagonist;   

DOI  :  10.1016/j.bmcl.2014.02.029

来源: Elsevier

【 摘 要 】

Chromones are a class of natural products found in almost every known terrestrial plant with over 4000 naturally occurring derivatives having been isolated and structurally elucidated. Recently, 5-hydroxy-2-(2-phenylethyl) chromone (5-HPEC), isolated from Imperata cylindrical, showed neuroprotective activity against glutamate induced excitotoxicity in primary cultures of rat cortical cells. In comparison to other naturally occurring neuroprotective chromones, 5-HPEC contains fewer hydroxyl groups. Here we report our most recent characterization on this interesting natural product against a number of CNS receptors for the purpose to identify the potential molecular targets that may be related to its biological activity. Based on our studies, including radiobinding assays, calcium flux functional assays and molecular modeling studies, 5-HPEC may represent a type of novel nonnitrogenous ligands to the 5-HT2B receptor. Published by Elsevier Ltd.

【 授权许可】

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