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11. 发明授权

US6028175A Mammalian methadone-specific opioid receptor 失效
标题翻译：哺乳动物美沙酮特异性阿片受体
公开(公告)号：US6028175A
公开(公告)日：2000-02-22
申请号：US170331
申请日：1998-10-13
申请人： David K. Grandy , James R. Bunzow , Olivier Civelli
发明人： David K. Grandy , James R. Bunzow , Olivier Civelli
IPC分类号： A61K39/00 , C07K14/705 , C12N15/12
CPC分类号： C07K14/705 , A61K39/00 , C07K2319/00 , C12N2799/023
摘要： 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.
摘要翻译：本发明涉及一种新型的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。

12. 发明授权

US5883226A Human dopamine receptor and its uses 失效
标题翻译：人类多巴胺受体及其用途
公开(公告)号：US5883226A
公开(公告)日：1999-03-16
申请号：US487811
申请日：1995-06-07
申请人： Olivier Civelli , Hubert Henri-Marie Van Tol
发明人： Olivier Civelli , Hubert Henri-Marie Van Tol
IPC分类号： C07K14/00 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12Q1/04 , C12Q1/68 , C12R1/91 , G01N33/50 , G01N33/94
CPC分类号： G01N33/9406 , C07K14/70571 , C12Q1/683 , G01N33/9413 , G01N2500/00 , G01N2500/10 , G01N2800/52
摘要： The present invention is directed toward the isolation, characterization and pharmacological use of the human D4 dopamine receptor. The nucleotide sequence of the gene corresponding to this receptor and alleleic variant thereof are provided by the invention. The invention also includes recombinant eukaryotic expression constructs capable of expressing the human D4 dopamine receptor in cultures of transformed eukaryotic cells. The invention provides cultures of transformed eukaryotic cells which synthesize the human D4 dopamine receptor, and methods for characterizing novel psychotropic compounds using such cultures.
摘要翻译：本发明涉及人D4多巴胺受体的分离，表征和药理学应用。对应于该受体的基因的核苷酸序列及其等位变体由本发明提供。本发明还包括能够在转化的真核细胞的培养物中表达人D4多巴胺受体的重组真核表达构建体。本发明提供合成人D4多巴胺受体的转化真核细胞的培养物，以及使用这种培养物表征新的精神药物的方法。

13. 发明授权

US5837809A Mammalian opioid receptor ligand and uses 失效
标题翻译：哺乳动物阿片受体配体及用途
公开(公告)号：US5837809A
公开(公告)日：1998-11-17
申请号：US514451
申请日：1995-08-11
申请人： David K. Grandy , James R. Bunzow , Olivier Civelli , Rainer Klaus Reinscheid , Hans-Peter Nothacker , Frederick James Monsma
发明人： David K. Grandy , James R. Bunzow , Olivier Civelli , Rainer Klaus Reinscheid , Hans-Peter Nothacker , Frederick James Monsma
IPC分类号： A61K38/00 , C07K14/665 , C07K7/08 , C07K14/705
CPC分类号： C07K14/665 , A61K38/00
摘要： The present invention relates to a novel mammalian opioid receptor protein and ligands that bind to such proteins. The invention is directed toward the isolation, characterization and pharmacological use of an endogenous ligand that specifically binds to a novel mammalian opioid receptor protein heterologously expressed in mammalian cells. The invention specifically provides the isolated peptide ligand and analogues, derivatives and variants thereof. The invention specifically provides tyrosine substitution variants of the peptide ligand that specifically bind to the opioid receptor and can be radioiodinated. Also provided are methods of making such peptide ligands and methods of using the ligands for diagnostic and therapeutic uses and for the identification of other naturally-occurring or synthetic opioid receptor ligands.
摘要翻译：本发明涉及新型的哺乳动物阿片受体蛋白质和与这些蛋白质结合的配体。本发明涉及特异性结合在哺乳动物细胞中异源表达的新型哺乳动物阿片受体蛋白的内源性配体的分离，表征和药理学应用。本发明特别提供了分离的肽配体及其类似物，衍生物和变体。本发明具体提供肽配体的酪氨酸取代变体，其特异性结合阿片受体并可以放射性碘化。还提供了制备这种肽配体的方法和使用配体用于诊断和治疗用途以及鉴定其它天然存在或合成的阿片受体配体的方法。

14. 发明授权

US5658783A Mammalian methadone-specific opioid receptor gene and uses 失效
标题翻译：哺乳动物美沙酮特异性阿片受体基因及用途
公开(公告)号：US5658783A
公开(公告)日：1997-08-19
申请号：US149093
申请日：1993-11-08
申请人： David K. Grandy , James R. Bunzow , Olivier Civelli
发明人： David K. Grandy , James R. Bunzow , Olivier Civelli
IPC分类号： A61K39/00 , C07K14/705 , C12N15/12 , C12N5/10
CPC分类号： C07K14/705 , A61K39/00 , C07K2319/00 , C12N2799/023
摘要： The present invention relates to a novel mammalian methadone-specific opioid receptor protein and genes that encode a such 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 or 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.
摘要翻译：本发明涉及一种新型的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大鼠同系物或哺乳动物美沙酮特异性阿片受体基因相对应的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。

15. 发明授权

US5594108A Human dopamine receptor and its uses 失效
标题翻译：人类多巴胺受体及其用途
公开(公告)号：US5594108A
公开(公告)日：1997-01-14
申请号：US333977
申请日：1994-11-03
申请人： Olivier Civelli , Hubert H. Van Tol
发明人： Olivier Civelli , Hubert H. Van Tol
IPC分类号： C07K14/00 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12Q1/04 , C12Q1/68 , C12R1/91 , G01N33/50 , G01N33/94
CPC分类号： G01N33/9406 , C07K14/70571 , C12Q1/683 , G01N33/9413 , G01N2500/00 , G01N2800/52
摘要： The present invention is directed toward the isolation, characterization and pharmacological use of the human D.sub.4 dopamine receptor. The nucleotide sequence of the gene corresponding to this receptor is provided by the invention. The invention also includes a recombinant eukaryotic expression vector capable of expressing the human D.sub.4 dopamine receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells which synthesize the human D.sub.4 dopamine receptor.
摘要翻译：本发明涉及人D4多巴胺受体的分离，表征和药理学应用。对应于该受体的基因的核苷酸序列由本发明提供。本发明还包括能够在转化的真核细胞和合成人D4多巴胺受体的转化真核细胞的培养物中表达人D4多巴胺受体的重组真核表达载体。

16. 发明授权

US5569601A Human dopamine receptor and its uses 失效
公开(公告)号：US5569601A
公开(公告)日：1996-10-29
申请号：US928611
申请日：1992-08-10
申请人： Olivier Civelli
发明人： Olivier Civelli
IPC分类号： C07K14/00 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12Q1/04 , C12Q1/68 , C12R1/91 , G01N33/50 , G01N33/94 , C12N5/00 , C07H17/00 , C12N15/00 , C12P21/06
CPC分类号： G01N33/9406 , C07K14/70571 , C12Q1/683 , G01N33/9413 , G01N2500/00 , G01N2500/10 , G01N2800/52
摘要： The present invention is directed toward the isolation, characterization and pharmacological use of the human D4 dopamine receptor. The nucleotide sequence of the gene corresponding to this receptor and alleleic variant thereof are provided by the invention. The invention also includes recombinant eukaryotic expression constructs capable of expressing the human D4 dopamine receptor in cultures of transformed eukaryotic cells. The invention provides cultures of transformed eukaryotic cells which synthesize the human D4 dopamine receptor, and methods for characterizing novel psychotropic compounds using such cultures.

17. 发明授权

US5516683A Human D4 dopamine receptor and its uses 失效
标题翻译：人类D4多巴胺受体及其用途
公开(公告)号：US5516683A
公开(公告)日：1996-05-14
申请号：US56051
申请日：1993-04-29
申请人： David K. Grandy , James R. Bunzow , Olivier Civelli , Hubert H.-M. Van Tol
发明人： David K. Grandy , James R. Bunzow , Olivier Civelli , Hubert H.-M. Van Tol
IPC分类号： C07K14/705 , C12Q1/68 , G01N33/94 , C12N15/12
CPC分类号： C07K14/70571 , C12Q1/683 , G01N33/9406 , G01N33/9413 , G01N2500/00 , G01N2800/52
摘要： The present invention is directed toward the isolation, characterization and pharmacological use of the human D4 dopamine receptor. The nucleotide sequence of the gene corresponding to this receptor and alleleic variants thereof are provided by the invention. The invention particularly provides recombinant eukaryotic expression constructs capable of expressing the human D4 dopamine receptor at useful levels in cultures of transformed eukaryotic cells. The invention provides cultures of transformed eukaryotic cells which synthesize such useful amounts of human D4 dopamine receptor protein, and methods for characterizing novel psychotropic compounds using such cultures.
摘要翻译：本发明涉及人D4多巴胺受体的分离，表征和药理学应用。对应于该受体的基因的核苷酸序列及其等位变体由本发明提供。本发明特别提供能够在转化的真核细胞的培养物中以有用水平表达人D4多巴胺受体的重组真核表达构建体。本发明提供合成这种有用量的人D4多巴胺受体蛋白质的转化真核细胞的培养物，以及使用这种培养物表征新的精神药物的方法。

18. 发明授权

US5441883A A3 adenosine receptor, DNA, and uses 失效
标题翻译： A3腺苷受体，DNA和用途
公开(公告)号：US5441883A
公开(公告)日：1995-08-15
申请号：US101435
申请日：1993-08-02
申请人： Olivier Civelli , Qun-Yong Zhou
发明人： Olivier Civelli , Qun-Yong Zhou
IPC分类号： A61K38/00 , C07K14/705 , C12N15/12
CPC分类号： C07K14/705 , A61K38/00
摘要： The present invention relates to a novel mammalian adenosine receptor. The invention is directed toward the isolation, characterization and pharmacological use of the rat A3 adenosine receptor, the gene corresponding to this receptor, a recombinant eukaryotic expression construct capable of expressing the rat A3 adenosine receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that synthesize the rat A3 adenosine receptor. The invention also provides methods for screening adenosine-receptor agonists and antagonists in vitro using preparations of the rat A3 adenosine receptor from such cultures of eukaryotic cells transformed with a recombinant eukaryotic expression construct comprising the rat A3 adenosine receptor gene.
摘要翻译：本发明涉及新型哺乳动物腺苷受体。本发明涉及大鼠A3腺苷受体（对应于该受体的基因）的分离，表征和药理学应用，能够在转化的真核细胞的培养物中表达大鼠A3腺苷受体的重组真核表达构建体，合成大鼠A3腺苷受体的真核细胞。本发明还提供了使用由包含大鼠A3腺苷受体基因的重组真核表达构建体转化的真核细胞的这种培养物中的大鼠A3腺苷受体的制备体外筛选腺苷受体激动剂和拮抗剂的方法。

19. 发明授权

US09012407B2 Therapies which act on neuropeptide S receptors 有权
标题翻译：作用于神经肽S受体的疗法
公开(公告)号：US09012407B2
公开(公告)日：2015-04-21
申请号：US11587444
申请日：2005-04-25
申请人： Olivier Civelli , Rainer K. Reinscheid , Yanling Xu
发明人： Olivier Civelli , Rainer K. Reinscheid , Yanling Xu
IPC分类号： A61K38/17 , A61K31/4985
CPC分类号： A61K31/4985 , A61K38/1709
摘要： Compositions and methods that act on Neuropeptide S receptors (NPSR) (also known as “TGR23” or “vasopressin receptor-related receptor 1 (VRR1)”) to cause desired effects in the bodies of human or animal subjects. Neuropeptide S (NPS) and other agonists of the NPSR may be administered to cause arousal, awakening, alertness, spontaneous movement, bronchoconstriction, contraction of bronchial smooth muscle or other effects. Antagonists of the NPSR may be administered to cause decreased arousal, decreased awakening, decreased alertness, decreased spontaneous movement, sleep, somnolence, sedation, anxiolytic effects, normalized sleep patterns, normalized sleep stages, increased duration of sleep, bronchodilation, relaxation of broncheal smooth muscle or other effects.
摘要翻译：作用于神经肽S受体（NPSR）（也称为“TGR23”或“加压素受体相关受体1（VRR1）”）的组合物和方法，以在人或动物受试者的身体中产生预期的效果。神经肽S（NPS）和NPSR的其它激动剂可以被施用以引起觉醒，觉醒，警觉，自发运动，支气管收缩，支气管平滑肌收缩或其它作用。可以施用NPSR的拮抗剂以引起觉醒降低，警觉性降低，自发运动降低，睡眠，嗜睡，镇静，抗焦虑作用，归一化睡眠模式，归一化睡眠阶段，睡眠增加持续时间，支气管扩张，放射支气管平滑肌肉或其他影响。

20. 发明申请

US20100056455A1 Therapies Which Act on Neuropeptide S Receptors 有权
标题翻译：对神经肽S受体的作用
公开(公告)号：US20100056455A1
公开(公告)日：2010-03-04
申请号：US11587444
申请日：2005-04-25
申请人： Olivier Civelli , Rainer K Reinscheld , Yanling Xu
发明人： Olivier Civelli , Rainer K Reinscheld , Yanling Xu
IPC分类号： A61K38/17 , A61P25/00 , C07K14/435
CPC分类号： A61K31/4985 , A61K38/1709
摘要： Compositions and methods that act on Neuropeptide S reseptors (NPSR) (also known as or “TGR23” or “vasopressin receptor-related receptor 1 (VRR1)”) to cause desired effects in the bodies of human or animal subjects. Neuropeptide S (NPS) and other agonists of the NPSR may be administered to cause arousal, awakening, alertness, spontaneous movement, bronchoconstriction, contraction of bronchial smooth muscle or other effects. Antagonists of the NPSR may be administered to cause decreased arousal, decreased awakening, decreased alertness, decreased spontaneous movement, sleep, somnolence, sedation, anxiolytic effects, normalized sleep patterns, normalized sleep stages, increased duration of sleep, bronchodilation, relaxation of broncheal smooth muscle or other effects.
摘要翻译：作用于神经肽S受体（NPSR）（也称为或“TGR23”或“加压素受体相关受体1（VRR1）”）的组合物和方法，以在人或动物受试者的身体中产生预期的效果。神经肽S（NPS）和NPSR的其它激动剂可以被施用以引起觉醒，觉醒，警觉，自发运动，支气管收缩，支气管平滑肌收缩或其它作用。可以施用NPSR的拮抗剂以引起觉醒降低，警觉性降低，自发运动降低，睡眠，嗜睡，镇静，抗焦虑作用，归一化睡眠模式，归一化睡眠阶段，睡眠增加持续时间，支气管扩张，放射支气管平滑肌肉或其他影响。

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