Pharmacokinetics of H002, a novel S1PR1 modulator, and its metabolites in rat blood using liquid chromatography-tandem mass spectrometry
A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of H002 and its phosphorylated metabolite, H002-P and hydroxylated metabolite H002-M, in rat blood. H001, an analogue of H002, was used as the interna...
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Elsevier,
2016-10-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_acb9d19822ca413ea064de3b3ffe3d3b | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Jiaqi Mi |e author |
| 700 | 1 | 0 | |a Manman Zhao |e author |
| 700 | 1 | 0 | |a Shu Yang |e author |
| 700 | 1 | 0 | |a Shuang Yang |e author |
| 700 | 1 | 0 | |a Jing Jin |e author |
| 700 | 1 | 0 | |a Xiaojian Wang |e author |
| 700 | 1 | 0 | |a Qiong Xiao |e author |
| 700 | 1 | 0 | |a Jinping Hu |e author |
| 700 | 1 | 0 | |a Yan Li |e author |
| 245 | 0 | 0 | |a Pharmacokinetics of H002, a novel S1PR1 modulator, and its metabolites in rat blood using liquid chromatography-tandem mass spectrometry |
| 260 | |b Elsevier, |c 2016-10-01T00:00:00Z. | ||
| 500 | |a 2211-3835 | ||
| 500 | |a 2211-3843 | ||
| 500 | |a 10.1016/j.apsb.2016.06.001 | ||
| 520 | |a A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of H002 and its phosphorylated metabolite, H002-P and hydroxylated metabolite H002-M, in rat blood. H001, an analogue of H002, was used as the internal standard. Blood samples were prepared by simple protein precipitation. The analytes and internal standard were separated on a Zorbax SB-C18 column with a gradient mobile phase consisting of methanol and water containing 0.1% formic acid at a flow rate of 0.2 mL/min with an operating temperature of 20 °C. The detection was performed on a triple quadrupole tandem mass spectrometer with positive electrospray ionization in multiple-reaction monitoring mode. Linear detection responses were obtained from 0.2-100 ng/mL for H002 and H002-M, while 0.5-100 ng/mL for H002-P. The intra- and inter-day precision (RSD%) was within 11.76%, with the accuracy (RE%) ranging from -9.84% to 9.12%. The analytes were shown to be stable during sample storage, preparation and analytic procedures. The method was applied to determine the pharmacokinetics of H002 in rats, and a preliminary study showed that the pharmacokinetics of H002 correlated with its biological effect on peripheral blood lymphocytes. | ||
| 546 | |a EN | ||
| 690 | |a S1P receptor | ||
| 690 | |a S1PR1 modulator | ||
| 690 | |a Sphingosine-1-phosphate | ||
| 690 | |a S1P analogue | ||
| 690 | |a Metabolite | ||
| 690 | |a LC-MS/MS | ||
| 690 | |a Pharmacokinetics | ||
| 690 | |a Periphery blood lymphocyte | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Acta Pharmaceutica Sinica B, Vol 6, Iss 6, Pp 576-583 (2016) | |
| 787 | 0 | |n http://www.sciencedirect.com/science/article/pii/S2211383515300435 | |
| 787 | 0 | |n https://doaj.org/toc/2211-3835 | |
| 787 | 0 | |n https://doaj.org/toc/2211-3843 | |
| 856 | 4 | 1 | |u https://doaj.org/article/acb9d19822ca413ea064de3b3ffe3d3b |z Connect to this object online. |