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    Neutral antagonists and use thereof in treating drug abuse
    1.
    发明授权
    Neutral antagonists and use thereof in treating drug abuse 失效
    中性拮抗剂及其在治疗药物滥用中的用途

    公开(公告)号：US06713488B2

    公开(公告)日：2004-03-30

    申请号：US10173337

    申请日：2002-06-14

    申请人： Wolfgang Sadée ,  Danxin Wang

    发明人： Wolfgang Sadée ,  Danxin Wang

    IPC分类号： A61K31485

    CPC分类号： A61K31/485

    摘要： The invention relates to the use of naltrexone and naloxone analogs, which are neutral antagonists at the &mgr; opioid receptor, for the treatment of drug dependency in a drug-dependent individual. Surprisingly, it has been found that administration of a therapeutically effect amount of the naloxone or naltrexone analogs described herein for the treatment of a drug dependency, can result in reduction of undesirable side effects resulting from current treatments using naloxone and naltrexone. For example, the treatment described herein can result in a reduction in the withdrawal symptoms and aversion encountered in the use of naloxone and naltrexone in the treatment of drug dependency. In addition, the naltrexone and naloxone analogs of the invention can be used for the treatment of pain in an individual in need thereof by modulating opoid pain treatment using neutral antagonists, for example, reversing respiratory depression withough causing other adverse effects. In addition, during chronic use of opioid drugs for pain therapy, neutral antagonists can be used to diminish constipation peripherally without effecting the central analgesic effects.

    摘要翻译： 本发明涉及在阿片样物质受体中作为中性拮抗剂的纳曲酮和纳洛酮类似物用于治疗依赖于药物的个体的药物依赖性。 令人惊奇的是，已经发现，治疗有效量的本文所述的纳洛酮或纳曲酮类似物的给药用于治疗药物依赖性可导致由使用纳洛酮和纳曲酮的当前治疗引起的不希望的副作用的减少。 例如，本文所述的治疗可导致使用纳洛酮和纳曲酮治疗药物依赖性时所引起的戒断症状和厌恶的减少。 此外，本发明的纳曲酮和纳洛酮类似物可以用于通过使用中性拮抗剂调节类固醇疼痛治疗来治疗有需要的个体的疼痛，例如逆转呼吸抑制而不引起其他副作用。 此外，在慢性使用阿片类药物进行疼痛治疗时，中性拮抗剂可用于周边地减少便秘而不影响中枢镇痛作用。