Clarke R L, Heckeler M L, Gambino A J, Daum S J, Harding H R, Pierson A K, Teiger D G, Pearl J, Shargel L D, Goehl T J
J Med Chem. 1978 Dec;21(12):1243-53. doi: 10.1021/jm00210a014.
(exo, exo)-2-Aryltropane-3-carboxylic esters of types 6, 7, and 10 lower circulating blood glucose levels by 60--80%. This activity is accompanied by an analgesic activity roughly equal to that of codeine. Both of these activities reside in the 1R enantiomer and extensive structure-activity studies failed to separate them. The specific opioid antagonist nalorphine blocks the analgesic activity but does not diminish the hypoglycemic action. Conformational integrity afforded by the ethylene bridge is neccessary for the observed activities.
6型、7型和10型的（外向，外向）-2-芳基托烷-3-羧酸酯可使循环血糖水平降低60%至80%。此活性伴有大致与可待因相当的镇痛活性。这两种活性均存在于1R对映体中，广泛的构效关系研究未能将它们分开。特异性阿片样物质拮抗剂纳洛啡可阻断镇痛活性，但不减弱降血糖作用。观察到的活性需要乙烯桥提供的构象完整性。
