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Administration study of recombinant human relaxin-2 in horse for doping control purpose.
Drug Testing and Analysis ( IF 2.9 ) Pub Date : 2020-01-13 , DOI: 10.1002/dta.2732
Wai Him Kwok 1 , Timmy L S Choi 1 , Gary N W Leung 1 , April S Y Wong 1 , Samuel K Yue 2 , Terence S M Wan 1 , Emmie N M Ho 1
Affiliation  

The insulin‐like peptide relaxin (RLX), an endogenous peptide hormone produced in human for pregnancy and reproduction, is also known to exert a range of physiological and pathological effects. Its use is banned in human sports, horseracing, and equestrian competitions due to its potential performance enhancing effect through vasodilation resulting in the increase of blood and oxygen supplies to muscles. Little is known about the biotransformation and elimination of RLX in horses. This paper describes an administration study of rhRLX‐2 and its elimination in horses, and the development of sensitive methods for the detection and confirmation of rhRLX‐2 in both horse plasma and urine by nano‐liquid chromatography/high resolution mass spectrometry (nano‐LC/HRMS) after immunoaffinity extraction with the objective of controlling the abuse of rhRLX‐2 in horses. The limits of detection in plasma and urine are 2 pg/mL and 5 pg/mL, respectively. Two thoroughbred geldings were each administered one dose of 10 mg rhRLX‐2 subcutaneously daily for 3 consecutive days. The rhRLX‐2 could be detected and confirmed in the plasma and urine samples collected 105 h and 80 h, respectively, after the last dose of administration. For doping control purposes, rhRLX‐2 ELISA could be used as a screening test to identify potential positive samples for further investigation using the nano‐LC/HRMS methods.

中文翻译:

重组人松弛素2在马中用于兴奋剂控制的给药研究。

胰岛素样肽松弛素(RLX)是人体内产生的一种用于妊娠和生殖的内源性肽激素,还具有多种生理和病理作用。由于其通过血管舒张的潜在性能增强作用,导致增加了向肌肉的血液和氧气供应,因此禁止在人类运动,赛马和马术比赛中使用它。关于马中RLX的生物转化和消除知之甚少。本文介绍了rhRLX-2的管理研究及其在马中的消除,并开发了用于亲和提取后通过纳米液相色谱/高分辨率质谱(nano-LC / HRMS)检测和确认马血浆和尿液中rhRLX-2敏感方法的方法,目的是控制rhRLX的滥用‐2在马匹中。血浆和尿液中的检出限分别为2 pg / mL和5 pg / mL。每天两次皮下注射两种纯种胶,每次连续10天,一次皮下注射一剂10 mg rhRLX-2。在最后一次给药后,分别在105 h和80 h收集的血浆和尿液样本中检测到并确认了rhRLX-2。出于掺杂控制的目的,rhRLX-2 ELISA可用作筛选测试,以鉴定潜在的阳性样品,以使用nano-LC / HRMS方法进行进一步研究。血浆和尿液中的检出限分别为2 pg / mL和5 pg / mL。每天两次皮下注射两种纯种胶,每次连续10天,一次皮下注射一剂10 mg rhRLX-2。在最后一次给药后,分别在105 h和80 h收集的血浆和尿液样本中检测到并确认了rhRLX-2。出于掺杂控制的目的,rhRLX-2 ELISA可用作筛选测试,以鉴定潜在的阳性样品,以使用nano-LC / HRMS方法进行进一步研究。血浆和尿液中的检出限分别为2 pg / mL和5 pg / mL。每天两次皮下注射两种纯种胶,每次连续10天,一次皮下注射一剂10 mg rhRLX-2。在最后一次给药后,分别在105 h和80 h收集的血浆和尿液样本中检测到并确认了rhRLX-2。出于掺杂控制的目的,rhRLX-2 ELISA可用作筛选测试,以鉴定潜在的阳性样品,以使用nano-LC / HRMS方法进行进一步研究。最后一剂给药后。出于掺杂控制的目的,rhRLX-2 ELISA可用作筛选测试,以鉴定潜在的阳性样品,以使用nano-LC / HRMS方法进行进一步研究。最后一剂给药后。出于掺杂控制的目的,rhRLX-2 ELISA可用作筛选测试,以鉴定潜在的阳性样品,以使用nano-LC / HRMS方法进行进一步研究。
更新日期:2020-01-13
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