マブチ　ミユキ   馬渕　美雪    所属   兵庫医科大学  薬学部 医療薬学科    職種   助教
言語種別	英語
発行・発表の年月	2017/07
形態種別	学術雑誌
査読	査読あり
標題	Synthesis of resveratrol derivatives as new analgesic drugs through desensitization of the TRPA1 receptor.
執筆形態	共著
掲載誌名	Bioorganic & medicinal chemistry letters
掲載区分	国外
巻・号・頁	27(14),pp.3167-3172
著者・共著者	Nakao Syuhei, Mabuchi Miyuki, Wang Shenglan, Kogure Yoko, Shimizu Tadashi, Noguchi Koichi, Tanaka Akito, Dai Yi
概要	A series of 31 resveratrol derivatives was designed, synthesized and evaluated for activation and inhibition of the TRPA1 channel. Most acted as activators and desensitizers of TRPA1 channels like resveratrol or allyl isothiocyanate (AITC). Compound 4z (HUHS029) exhibited higher inhibitory activity than resveratrol with an IC50 value of 16.1μM. The activity of 4z on TRPA1 was confirmed in TRPA1-expressing HEK293 cells, as well as in rat dorsal root ganglia neurons by a whole cell patch clamp recording. Furthermore, pretreatment with 4z exhibited an analgesic effect on AITC-evoked TRPA1-related pain behavior in vivo.
DOI	10.1016/j.bmcl.2017.05.025
ISSN	1464-3405
PMID	28576617