Preparation and biological properties of biotinylated PhTX derivatives

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

Index: 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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Citation Number: 19

Abstract

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 ...