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    • 94. 发明公开
    • Novel conjugates of opioids and endogenous carriers
    • 阿片样物质内分泌素trägerproteinen
    • EP1167383A1
    • 2002-01-02
    • EP01121557.1
    • 1998-11-06
    • Conjuchem, Inc.
    • Ezrin, Alan M.Bridon, Dominique P.Holmes, Darren L.Milner, Peter
    • C07K14/665C07K14/70A61K47/48
    • A61K49/0056A61K38/00A61K47/643A61K47/6901C07K14/665
    • Conjugates are prepared from antinociceptive agents, particularly opioids or opioid analogs, more particularly dynorphins, endorphins, deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably a blood cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient may be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro ) and introducing that conjugate to the patient's vascular system.
    • 通过将所述抗伤害感受剂与提供能够与血液成分(优选血液)反应的功能反应性基团的材料组合,由抗感受伤害剂,特别是阿片样物质或阿片样物质类似物,更特别是强啡肽,内啡肽,去角质素,脑啡肽或其类似物制备缀合物 细胞或蛋白质)。 所述缀合物允许延长抗伤害感受剂的治疗寿命。 可以向患者施用以缓解疼痛,产生镇痛作用或辅助戒毒的情况,并且也可以用作受体活性的探针。 对患者的施用可以在体内或体外制备,并且可以通过将包含反应性官能团的衍生物引入患者的血管系统中或者从外部(或体外)引入该缀合物并将该缀合物引入到 病人的血管系统。