Wentland M P, Lou R, Dehnhardt C M, Duan W, Cohen D J, Bidlack J M
Department of Chemistry, Rensselaer Polytechnic Institute, 110 8th Street, 12180, Troy, NY, USA.
Bioorg Med Chem Lett. 2001 Jul 9;11(13):1717-21. doi: 10.1016/s0960-894x(01)00278-5.
In response to the unexpectedly high affinity for opioid receptors observed in a novel series of cyclazocine analogues where the prototypic 8-OH was replaced by a carboxamido group, we have prepared the corresponding 3-CONH(2) analogues of morphine and naltrexone. High affinity (K(i)=34 and 1.7nM) for mu opioid receptors was seen, however, the new targets were 39- and 11-fold less potent than morphine and naltrexone, respectively.
在一系列新型环唑辛类似物中，当原型的8-OH被羧酰胺基团取代时，观察到对阿片受体具有出乎意料的高亲和力，为此我们制备了吗啡和纳曲酮相应的3-CONH(2)类似物。虽然观察到对μ阿片受体具有高亲和力（K(i)=34和1.7nM），但新靶点的效力分别比吗啡和纳曲酮低39倍和11倍。
