期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 161, 期 -, 页码 239-251出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.09.070
关键词
CBR ligands; CB2R agonists; Skin inflammation; Chemokine release
资金
- MIUR Progetto Dipartimenti di Eccellenza 2018-2022
A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, 1, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist 8g, showing the best balance between receptor affinity and selectivity, was tested in vitro in an experimental model of allergic contact dermatitis and proved to be able to block the release of MCP-2 in HaCaT cells at 10 mu M concentration. (C) 2018 Elsevier Masson SAS. All rights reserved.
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