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    • 9. 发明授权
    • Mammalian methadone-specific opioid receptor gene and uses
    • 哺乳动物美沙酮特异性阿片受体基因及用途
    • US06280973B1
    • 2001-08-28
    • US09510473
    • 2000-02-22
    • David K. GrandyJames R. BunzowOlivier Civelli
    • David K. GrandyJames R. BunzowOlivier Civelli
    • C12P2106
    • C07K14/705A61K39/00C07K2319/00C12N2799/023
    • The present invention relates to a novel-mammalian methadone-specific opioid receptor protein and genes that encode such a protein. The invention is directed toward the isolation, characterization and pharmacological use of mammalian methadone-specific opioid receptor proteins. The invention specifically provides isolated complementary DNA copies of mRNA corresponding to the rat homologue of the mammalian methadone-specific opioid receptor gene. Also provided are recombinant expression constructs capable of expressing the mammalian methadone-specific opioid receptor genes of the invention in cultures of transformed prokaryotic and eukaryotic cells, as well as such cultures of transformed cells that synthesize the mammalian methadone-specific opioid receptor proteins encoded therein. The invention also provides methods for screening compounds in vitro that are capable of binding to the mammalian methadone-specific opioid receptor proteins of the invention, and further characterizing the binding properties of such compounds in comparison with known opioid receptor agonists and antagonists.
    • 本发明涉及新型哺乳动物美沙酮特异性阿片受体蛋白质和编码这种蛋白质的基因。 本发明涉及哺乳动物美沙酮特异性阿片受体蛋白的分离,表征和药理学应用。 本发明具体提供了与哺乳动物美沙酮特异性阿片受体基因的大鼠同系物相对应的mRNA的分离的互补DNA拷贝。 还提供能够在转化的原核和真核细胞的培养物中表达本发明的哺乳动物美沙酮特异性阿片受体基因以及合成其中编码的哺乳动物美沙酮特异性阿片受体蛋白质的转化细胞的这种培养物的重组表达构建体。 本发明还提供了在体外筛选能够结合本发明的哺乳动物美沙酮特异性阿片受体蛋白质的方法,并且与已知的阿片受体激动剂和拮抗剂相比进一步表征了这些化合物的结合性质。