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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。进一步研究正在进行
OBJECTIVE To design and synthesize 3-tetrahydrofurylmethylbenzalzan analogues with similar affinity to cyclozocine for opioid receptors and long duration of action in vivo. Method 8 Trifluoromethanesulfonate 3 Tetrahydrofuran Methylbenzophenone The target compound was obtained by catalytic ammonification, and the affinity of the target compound was determined. Results 8-amino and 8-phenylalanine compounds showed lower affinity to μ, δ and κ receptors in vitro than the corresponding 8-hydroxy compounds. Conclusion The target compounds have relatively low affinity in vitro receptors, but this result still can not fully explain the role of the target compounds in vivo and their potential for drug addiction treatment. Further research is ongoing