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    • 2. 发明授权
    • Methods of identifying and ADP-glucose receptor ligand, agonist or antagonist
    • 识别ADP-葡萄糖受体配体,激动剂或拮抗剂的方法
    • US06790608B2
    • 2004-09-14
    • US09780576
    • 2001-02-09
    • Olivier CivelliHans-Peter NothackerZhiwei WangRainer Reinscheid
    • Olivier CivelliHans-Peter NothackerZhiwei WangRainer Reinscheid
    • C12Q100
    • G01N33/66
    • The present invention provides an isolated nucleic acid molecule containing a nucleotide sequence which encodes an ADP-glucose receptor, and isolated polynucleotides therefrom. Also provided is an isolated ADP-glucose receptor polypeptide, an isolated immunogenic peptide therefrom, and antibodies specific therefor. The invention also provides a method of identifying an ADP-glucose receptor agonist or antagonist, by contacting an ADP-glucose receptor with one or more candidate compounds under conditions suitable for detection of a G-protein coupled signal in response to ADP-glucose, and identifying a candidate compound that alters production of the signal. Further provided is a method of identifying an ADP-glucose receptor ligand, by contacting an ADP-glucose receptor with one or more candidate compounds under conditions suitable for detecting selective binding of ADP-glucose to ADP-glucose receptor, and identifying a candidate compound that selectively binds the ADP-glucose receptor. Also provided are methods of diagnosing or determining susceptibility to ADP-glucose receptor associated conditions, by detecting in a sample from the individual expression of ADP glucose receptor nucleic acid molecules or polypeptides.
    • 本发明提供了分离的核酸分子,其含有编码ADP-葡萄糖受体的核苷酸序列及其分离的多核苷酸。 还提供了分离的ADP-葡萄糖受体多肽,其中分离的免疫原性肽及其特异性抗体。 本发明还提供了通过在适于检测响应于ADP-葡萄糖的G蛋白偶联信号的条件下使ADP-葡萄糖受体与一种或多种候选化合物接触来鉴定ADP-葡萄糖受体激动剂或拮抗剂的方法,以及 识别改变信号产生的候选化合物。 进一步提供的是通过在适于检测ADP-葡萄糖与ADP-葡萄糖受体的选择性结合的条件下将ADP-葡萄糖受体与一种或多种候选化合物接触并鉴定候选化合物来鉴定ADP-葡萄糖受体配体的方法 选择性结合ADP-葡萄糖受体。 还提供了通过在来自ADP葡萄糖受体核酸分子或多肽的个体表达的样品中检测来诊断或确定对ADP-葡萄糖受体相关病症易感性的方法。
    • 3. 发明授权
    • Methods of identifying compounds for controlling absence seizures in a mammal relating to prolactin-releasing peptide(PrRP)
    • 识别用于控制哺乳动物中与催乳素释放肽(PrRP)有关的癫痫发作的化合物的方法
    • US06383764B1
    • 2002-05-07
    • US09560915
    • 2000-04-28
    • Olivier CivelliSteven Lin
    • Olivier CivelliSteven Lin
    • G01N3353
    • G01N33/74A61K31/00
    • The invention provides a substantially pure Prolactin Releasing Peptide (PrRP) functional analog which suppresses absence seizures in a mammal, and related pharmaceutical compositions. The invention also provides a method of controlling absence seizures in a mammal, by administering to a mammal susceptible to absence seizures an effective amount of PrRP or a PrRP functional analog. Also provided are methods of identifying a compound that modulates AMPA receptor signaling in a mammal, by providing a compound that is a PrRP or PrRP functional analog, and determining the ability of the compound to modulate AMPA receptor signaling. The invention also provides methods of identifying a compound for controlling absence seizures in a mammal, by providing a compound that is a PrRP or PrRP functional analog, and determining the ability of the compound to control absence seizures in a mammal. Also provided are pharmaceutical compositions for controlling absence seizures in a mammal. The compositions and related methods contain a compound identified by the methods of the invention as a compound that modulates AMPA receptor signaling or as a compound that controls absence seizures.
    • 本发明提供了基本上纯的催乳素释放肽(PrRP)功能类似物,其抑制哺乳动物的不存在发作,以及相关的药物组合物。 本发明还提供了一种控制哺乳动物不存在癫痫发作的方法,该方法通过给予感染不发作的哺乳动物有效量的PrRP或PrRP功能性类似物。 还提供了通过提供作为PrRP或PrRP功能类似物的化合物以及测定化合物调节AMPA受体信号传导的能力来鉴定调节哺乳动物AMPA受体信号传导的化合物的方法。 本发明还提供了通过提供PrRP或PrRP功能类似物的化合物以及确定化合物控制哺乳动物中不存在癫痫发作的能力来鉴定用于控制哺乳动物中不存在发作的化合物的方法。 还提供了用于控制哺乳动物中不存在癫痫发作的药物组合物。 组合物和相关方法含有通过本发明的方法鉴定的化合物,其作为调节AMPA受体信号传导的化合物或作为控制不发作的化合物。
    • 5. 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。
    • 7. 发明授权
    • Mammalian methadone-specific opioid receptor and uses in binding assays
    • 哺乳动物美沙酮特异性阿片受体和结合测定中的用途
    • US5821067A
    • 1998-10-13
    • US911245
    • 1997-08-15
    • David K. GrandyJames R. BunzowOlivier Civelli
    • David K. GrandyJames R. BunzowOlivier Civelli
    • A61K39/00C07K14/705C12N15/12C12Q1/02
    • C07K14/705A61K39/00C07K2319/00C12N2799/023
    • The present invention relates to a novel mammalian met one-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.
    • 本发明涉及一种新型哺乳动物遇到的一种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。
    • 10. 发明授权
    • Screening and therapeutic methods for promoting wakefulness and sleep
    • 用于促进觉醒和睡眠的筛查和治疗方法
    • US06884596B2
    • 2005-04-26
    • US09932161
    • 2001-08-17
    • Olivier CivelliSteven Lin
    • Olivier CivelliSteven Lin
    • A61K31/00A61P5/02A61P5/04A61P25/08G01N33/74G01N33/53A61K38/00G01N33/566G01N33/567
    • G01N33/74A61K31/00
    • The invention provides methods of screening for a compound for promoting wakefulness in a mammal. The method is practiced by providing a compound that is a PrRP receptor agonist and determining the ability of the compound to promote wakefulness. Also provided by the invention are methods of screening for a compound for promoting sleep in a mammal. The methods are practiced by providing a compound that is a PrRP receptor antagonist and determining the ability of the compound to promote sleep. In addition, the invention provides a method of promoting wakefulness in a mammal. The method is practiced by administering to a mammal an effective amount of a PrRP receptor agonist. The invention further provides a method of promoting sleep in a mammal. The method is practiced by administering to a mammal an effective amount of a PrRP receptor antagonist.
    • 本发明提供筛选用于促进哺乳动物觉醒的化合物的方法。 该方法通过提供作为PrRP受体激动剂的化合物并确定化合物促进觉醒的能力来实施。 本发明还提供筛选用于促进哺乳动物睡眠的化合物的方法。 该方法通过提供作为PrRP受体拮抗剂的化合物并确定化合物促进睡眠的能力来实施。 此外,本发明提供了一种促进哺乳动物的觉醒的方法。 该方法通过向哺乳动物施用有效量的PrRP受体激动剂来实施。 本发明还提供一种促进哺乳动物睡眠的方法。 该方法通过向哺乳动物施用有效量的PrRP受体拮抗剂来实施。