MDR-1-INHIBITION AND CYP3A ACTIVITY

MDR-1 抑制和 CYP3A 活性

• 批准号: 7375662
• 负责人: ALASTAIR J. J. WOOD
• 金额: $ 1.43万
• 依托单位: VANDERBILT UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-12-01 至 2006-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7375662
• 关键词: MDR; INHIBITION; CYP3A; ACTIVITY

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Our hypothesis is that MDR1 activity may affect the ERBT but not the midazolam clearance, and thus confound CYP3A assessment by the ERBT. The purpose of our study is to demonstrate that inhibition of MDR1 activity by the investigational MDR1 inhibitor tariquidar/XR-9576 (Xenova Ltd., UK) will affect the ERBT but not midazolam's disposition, possibly explaining the disparate results between these two assays for the determination of CYP3A activity.

该子项目是利用 NIH/NCRR 资助的中心拨款提供的资源的众多研究子项目之一。子项目和研究者 (PI) 可能已从另一个 NIH 来源获得主要资金，因此可以在其他 CRISP 条目中得到体现。列出的机构是中心的机构，不一定是研究者的机构。我们的假设是，MDR1 活性可能影响 ERBT，但不会影响咪达唑仑清除率，从而混淆 ERBT 的 CYP3A 评估。我们研究的目的是证明，研究中的 MDR1 抑制剂 tariquidar/XR-9576（Xenova Ltd.，英国）对 MDR1 活性的抑制会影响 ERBT，但不会影响咪达唑仑的处置，这可能解释了这两种测定 CYP3A 活性的测定之间的不同结果。