14-烷氧基吗啡喃的新型腙、肟、卡巴腙和氨基脲衍生物的阿片样物质结合谱

Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.

作者信息

Monory K, Greiner E, Sartania N, Sallai L, Pouille Y, Schmidhammer H, Hanoune J, Borsodi A

机构信息

Institute of Biochemistry, Biological Research Center, Hungarian Academy of Sciences, Szeged.

出版信息

Life Sci. 1999;64(22):2011-20. doi: 10.1016/s0024-3205(99)00148-4.

DOI:10.1016/s0024-3205(99)00148-4

PMID:10374926

Abstract

Several hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxycodeinones and 14-alkoxydihydrocodeinones were synthesised [1] and characterised in in vitro radioligand binding assays in rat brain membrane preparations. The tested compounds show the highest affinity for the mu opioid binding sites and most of them have agonist character. Subtype analysis of the binding shows mu2 specificity. However, some of these ligands are able to block partially (40-60%) the high affinity (putative mu1) opioid binding sites while all of them act as reversible ligands at the low affinity (putative mu2) sites.

摘要

合成了14-烷氧基可待因酮和14-烷氧基二氢可待因酮的几种腙、肟、卡巴腙和氨基脲衍生物[1]，并在大鼠脑膜制剂的体外放射性配体结合试验中对其进行了表征。所测试的化合物对μ阿片受体结合位点表现出最高亲和力，且其中大多数具有激动剂特性。结合的亚型分析显示具有μ2特异性。然而，其中一些配体能够部分阻断（40%-60%）高亲和力（假定为μ1）阿片受体结合位点，而它们在低亲和力（假定为μ2）位点均作为可逆配体起作用。