School of Pharmacy, Kitasato University, Tokyo, Japan.
Bioorg Med Chem Lett. 2012 Apr 15;22(8):2689-92. doi: 10.1016/j.bmcl.2012.03.001. Epub 2012 Mar 8.
A novel opioid ligand possessing a stable and cyclic imine 16 and its derivatives with an azabicyclo[2.2.2]octane skeleton were synthesized. The imine 16 showed higher affinity for the μ receptor than compound 21 with an oxabicyclo[2.2.2]octane skeleton. Azabicyclo[2.2.2]octane derivative 18d with a cyclopropylmethyl group on the 8-nitrogen showed the highest affinity for the μ receptor among the synthesized derivatives.
合成了一种具有稳定环状亚胺 16 的新型阿片样配体及其具有氮杂双环[2.2.2]辛烷骨架的衍生物。与具有氧杂双环[2.2.2]辛烷骨架的化合物 21 相比，亚胺 16 对 μ 受体具有更高的亲和力。在合成的衍生物中，8-位氮上带有环丙甲基的氮杂双环[2.2.2]辛烷衍生物 18d 对 μ 受体具有最高的亲和力。
