Preparation and biological properties of biotinylated PhTX derivatives

M Hashimoto, Y Liu, K Fang, H Li, G Campiani…

文献索引：Hashimoto, Masaru; Liu, Ying; Fang, Kan; Li, Hong-Yu; Campiani, Giuseppe; Nakanishi, Koji Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 6 p. 1181 - 1194

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被引用次数: 19

摘要

We report the synthesis of several highly functionalized biotinylated philanthotoxin (PhTX) analogues (7, 8, 10, 13–16) designed on the basis of earlier structure–activity relationship studies. Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range according to an inhibition assay using 3H- thienylcyclohexyl-piperidine (TCP). A patch clamp functional assay gave comparable ...