8-氨基-3-四氢呋喃甲基苯并吗吩烷的合成及药理活性(英文)

Synthesis and pharmacology of 8-amino-3-[(tetrahydro-2- furanyl)methyl] benzomorphan

目的 设计并合成与环佐辛有类似的阿片受体亲和活性、在体内具有较长作用时间的 3 四氢呋喃甲基苯并吗吩烷类似物。方法 8 三氟甲磺酸酯 3 四氢呋喃甲基苯并吗吩烷经催化氨化制得目标物 ,对目标物进行受体亲和力测定。结果 8 氨基及 8 苯氨基化合物在体外与 μ ,δ和κ受体的亲和力均较相应的 8 羟基化合物低。 结论 目标化合物的体外受体亲和力相对较低 ,但此结果尚不能完全说明其在体内的作用情况及其可否用于毒品成瘾的治疗。

Aim To design and synthesize new chiral 8 (substituted)amino analogues of 3 [(tetrahydro 2 furanyl)methyl] benzomorphans, to expand knowledge of the structure activity relationship(SAR) for 8 aminobenzomorphan. Methods Target compounds were synthesized from the 8 triflate of the optically active 3 [(tetrahydro 2 furanyl)methyl] 2,6 methano benzomorphans using Pd catalyzed aminations. Opioid receptor binding experiments were performed to evaluate their biological activities. Results Both ...