摘要Natural product bufotenine (5) which could be isolated from Venenum Bufonis,has been widely used as a tool in cent-ral nervous system (CNS) studies.We present here its quaternary ammonium salt (6) which was synthesized with high yields using 5-benzyloxyindole as raw materials,and we firstly discover its analgesic effects in vivo.The analgesic evaluation showed that com-pounds 5 and 6 had stronger effects on the behavior of formalin induced pain in mice.Moreover,the combination of compound 6 and morphine has a synergistic effect.We intended to explain the molecular mechanism of this effect.Therefore,36 analgesic-related tar-gets (including 15 G protein-coupled receptors,6 enzymes,13 ion channels,and 2 others) were systemically evaluated using reverse docking.The results indicate that bufotenine and its derivatives are closely related to acetyl cholinesterase (AChE) or α4β2 nicotinic acetylcholine receptor (nAChR).This study provides practitioners a new insight of analgesic effects.