N-methylquinine

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 金鸡纳生物碱
• 英文名称: N-methylquinine
• 英文别名: (R)-[(2S,4S,5R)-5-ethenyl-1-methyl-1-azoniabicyclo[2.2.2]octan-2-yl]-(6-methoxyquinolin-4-yl)methanol
• 化学式: C₂₁H₂₇N₂O₂
• 分子量: 339.458
• InChiKey: SJTSZVLGFLZBFK-KBYCNLJVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  42.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  碘甲烷 、 奎宁 生成 N-methylquinine
  参考文献：
  名称：

  Stereoselective transport of hydrophilic quaternary drugs by humanMDR1and ratMdr1bP-glycoproteins

  摘要：

  本研究旨在评估和比较人类 **MDR1**-、大鼠 **Mdr1b**- 和 **Mdr2**-P-糖蛋白运输疏水性季铵药物的能力。运输研究采用从过表达 **MDR1**、**Mdr1b** 或 **Mdr2** 的昆虫细胞中分离的血浆膜小泡进行。 我们使用了奎尼丁和金鸡纳碱这组对映异构体的 **N**-甲基化衍生物（单季铵化合物 **N**-甲基奎尼丁和 **N**-甲基金鸡纳碱）作为模型底物。已知的 **MDR1** 底物长春新碱用作参考。 我们观察到所有研究药物均能通过 **MDR1**- 和 **Mdr1b** 表达小泡的 ATP 依赖性摄取作用。**Mdr2** 无法运输这些化合物。**MDR1**- 和 **Mdr1b** 介导的运输具有饱和性，且可被多种药物（包括 PSC-833）抑制。 对于 **MDR1** 和 **Mdr1b**，**N**-甲基奎尼丁的最大速度与米氏常数的比值（或清除率）均高于 **N**-甲基金鸡纳碱。这种立体选择性差异也可通过两种异构体的抑制实验得到证实。 通过比较标准化清除率，我们发现人类 **MDR1** 在运输测试底物方面的效率高于大鼠 **Mdr1b**。 总之，我们的结果表明：**MDR1** 和 **Mdr1b**（而非 **Mdr2**）能够运输单季铵模型药物；两者均对这些阳离子表现出立体特异性；且人类 **MDR1** 在运输这些阳离子方面比其大鼠同源物 **Mdr1b** 更为高效。 *British Journal of Pharmacology* (2002) **135**, 1685–1694; doi: [10.1038/sj.bjp.0704620](https://doi.org/10.1038/sj.bjp.0704620)

  DOI：

  10.1038/sj.bjp.0704620

文献信息

• Polymorphisms in the human genes for OCT1 and their use in diagnostic and therapeutic applications
  申请人：PGXHealth, LLC

  公开号：EP2319866A2

  公开（公告）日：2011-05-11

  The present invention relates to a polymorphic OCT1 polynucleotide. Moreover, the invention relates to genes or vectors comprising the polynucleotides of the invention and to a host cell genetically engineered with the polynucleotide or gene of the invention. Further, the invention relates to methods for producing molecular variant polypeptides or fragments thereof, methods for producing cells capable of expressing a molecular variant polypeptide and to a polypeptide or fragment thereof encoded by the polynucleotide or the gene of the invention or which is obtainable by the method or from the cells produced by the method of the invention. Furthermore, the invention relates to an antibody which binds specifically the polypeptide of the invention. Moreover, the invention relates to a transgenic non-human animal. The invention also relates to a solid support comprising one or a plurality or the above mentioned polynucleotides, genes, vectors, polypeptides, antibodies or host cells. Furthermore, methods of identifying a polymorphism, identifying and obtaining a pro-drug or drug or an inhibitor are also encompassed by the present invention. In addition, the invention relates to methods for producing of a pharmaceutical composition and to methods of diagnosing a disease. Further, the invention relates to a method of detection of the polynucleotide of the invention. Furthermore, comprised by the present invention are a diagnostic and a pharmaceutical composition. Even more, the invention relates to uses of the polynucleotides, genes, vectors, polypeptides or antibodies of the invention. Finally, the invention relates to a diagnostic kit.

  本发明涉及一种多态 OCT1 多核苷酸。此外，本发明还涉及包含本发明多核苷酸的基因或载体，以及用本发明多核苷酸或基因进行遗传工程的宿主细胞。此外，本发明还涉及生产分子变异多肽或其片段的方法、生产能够表达分子变异多肽的细胞的方法以及由本发明多核苷酸或基因编码的多肽或其片段，或可通过本发明方法获得或从本发明方法生产的细胞中获得的多肽或其片段。此外，本发明还涉及一种能特异性结合本发明多肽的抗体。此外，本发明还涉及一种转基因非人类动物。本发明还涉及一种包含一种或多种上述多核苷酸、基因、载体、多肽、抗体或宿主细胞的固体支持物。此外，本发明还包括鉴定多态性、鉴定和获得原药或药物或抑制剂的方法。此外，本发明还涉及药物组合物的生产方法和疾病诊断方法。此外，本发明还涉及本发明多核苷酸的检测方法。此外，本发明还包括一种诊断方法和一种药物组合物。此外，本发明还涉及本发明的多核苷酸、基因、载体、多肽或抗体的用途。最后，本发明还涉及一种诊断试剂盒。
• Polymorphisms in the human genes for oct1 and their use in diagnostic and therapeutic applications
  申请人：Kerb Reinhold

  公开号：US20060122372A1

  公开（公告）日：2006-06-08

  The present invention relates to a polymorphic OCT1 polynucleotide. Moreover, the invention relates to genes or vectors comprising the polynucleotides of the invention and to a host cell genetically engineered with the polynucleotide or gene of the invention. Further, the invention relates to methods for producing molecular variant polypeptides or fragments thereof, methods for producing cells capable of expressing a molecular variant polypeptide and to a polypeptide or fragment thereof encoded by the polynucleotide or the gene of the invention or which is obtainable by the method or from the cells produced by the method of the invention. Furthermore, the invention relates to an antibody which binds specifically the polypeptide of the invention. Moreover, the invention relates to a transgenic non-human animal. The invention also relates to a solid support comprising one or a plurality of the above mentioned polynucleotides, genes, vectors, polypeptides, antibodies or host cells. Furthermore, methods of identifying a polymorphism, identifying and obtaining a pro-drug or drug or an inhibitor are also encompassed by the present invention. In addition, the invention relates to methods for producing of a pharmaceutical composition and to methods of diagnosing a disease. Further, the invention relates to a method of detection of the polynucleotide of the invention. Furthermore, comprised by the present invention are a diagnostic and a pharmaceutical composition. Even more, the invention relates to uses of the polynucleotides, genes, vectors, polypeptides or antibodies of the invention. Finally, the invention relates to a diagnostic kit.

  本发明涉及一种多态 OCT1 多核苷酸。此外，本发明还涉及包含本发明多核苷酸的基因或载体，以及用本发明多核苷酸或基因进行遗传工程的宿主细胞。此外，本发明还涉及生产分子变异多肽或其片段的方法、生产能够表达分子变异多肽的细胞的方法以及由本发明多核苷酸或基因编码的多肽或其片段，或可通过本发明方法获得或从本发明方法生产的细胞中获得的多肽或其片段。此外，本发明还涉及一种能特异性结合本发明多肽的抗体。此外，本发明还涉及一种转基因非人类动物。本发明还涉及一种包含一种或多种上述多核苷酸、基因、载体、多肽、抗体或宿主细胞的固体支持物。此外，本发明还包括鉴定多态性、鉴定和获得原药或药物或抑制剂的方法。此外，本发明还涉及药物组合物的生产方法和疾病诊断方法。此外，本发明还涉及本发明多核苷酸的检测方法。此外，本发明还包括一种诊断方法和一种药物组合物。此外，本发明还涉及本发明的多核苷酸、基因、载体、多肽或抗体的用途。最后，本发明还涉及一种诊断试剂盒。
• COMBINATIONS OF BETA-LACTAM COMPOUNDS AND PROBENECID AND USES THEREOF
  申请人：Iterum Therapeutics International Limited

  公开号：EP3801486A1

  公开（公告）日：2021-04-14
• Polymorphisms in the human genes for OCT 1 and their use in diagnostic and therapeutic applications
  申请人：Kerb Reinhold

  公开号：US20090061452A1

  公开（公告）日：2009-03-05

  The present invention relates to a polymorphic OCT1 polynucleotide. Moreover, the invention relates to genes or vectors comprising the polynucleotides of the invention and to a host cell genetically engineered with the polynucleotide or gene of the invention. Further, the invention relates to methods for producing molecular variant polypeptides or fragments thereof, methods for producing cells capable of expressing a molecular variant polypeptide and to a polypeptide or fragment thereof encoded by the polynucleotide or the gene of the invention or which is obtainable by the method or from the cells produced by the method of the invention. Furthermore, the invention relates to an antibody which binds specifically the polypeptide of the invention. Moreover, the invention relates to a transgenic non-human animal. The invention also relates to a solid support comprising one or a plurality of the above mentioned polynucleotides, genes, vectors, polypeptides, antibodies or host cells. Furthermore, methods of identifying a polymorphism, identifying and obtaining a pro-drug or drug or an inhibitor are also encompassed by the present invention. In addition, the invention relates to methods for producing of a pharmaceutical composition and to methods of diagnosing a disease. Further, the invention relates to a method of detection of the polynucleotide of the invention. Furthermore, comprised by the present invention are a diagnostic and a pharmaceutical composition. Even more, the invention relates to uses of the polynucleotides, genes, vectors, polypeptides or antibodies of the invention. Finally, the invention relates to a diagnostic kit.
• POLYMORPHISMS IN THE HUMAN GENES FOR OCT1 AND THEIR USE IN DIAGNOSTIC AND THERAPEUTIC APPLICATIONS
  申请人：Kerb Reinhold

  公开号：US20100009366A1

  公开（公告）日：2010-01-14

  The present invention relates to a polymorphic OCT1 polynucleotide. Moreover, the invention relates to genes or vectors comprising the polynucleotides of the invention and to a host cell genetically engineered with the polynucleotide or gene of the invention. Further, the invention relates to methods for producing molecular variant polypeptides or fragments thereof, methods for producing cells capable of expressing a molecular variant polypeptide and to a polypeptide or fragment thereof encoded by the polynucleotide or the gene of the invention or which is obtainable by the method or from the cells produced by the method of the invention. Furthermore, the invention relates to an antibody which binds specifically the polypeptide of the invention. Moreover, the invention relates to a transgenic non-human animal. The invention also relates to a solid support comprising one or a plurality of the above mentioned polynucleotides, genes, vectors, polypeptides, antibodies or host cells. Furthermore, methods of identifying a polymorphism, identifying and obtaining a pro-drug or drug or an inhibitor are also encompassed by the present invention. In addition, the invention relates to methods for producing of a pharmaceutical composition and to methods of diagnosing a disease. Further, the invention relates to a method of detection of the polynucleotide of the invention. Furthermore, comprised by the present invention are a diagnostic and a pharmaceutical composition. Even more, the invention relates to uses of the polynucleotides, genes, vectors, polypeptides or antibodies of the invention. Finally, the invention relates to a diagnostic kit.