Pharmacokinetic and metabolic studies of ADTM: a novel danshensu derivative confers cardioprotection by HPLC-UV and LC-MS/MS was written by Li, Sai;Shan, Luchen;Zhang, Zaijun;Li, Wei;Liao, Kaiyi;Li, Sha;Sheng, Xiaoyan;Yu, Pei;Wang, Yuqiang. And the article was included in Journal of Chromatographic Science in 2015.Category: pyrazines This article mentions the following:
(R)-(3,5,6-Trimethylpyrazinyl) methyl-2-acetoxy-3-(3,4-diacetoxyphenyl) propanoate (ADTM) is a novel Danshensu (DSS) derivative regarded as a potential new agent for the treatment of myocardial ischemia. A validated high performance liquid chromatog. (HPLC) approach with a detection limit of 5 ng/mL was used for pharmacokinetic evaluation of ADTM in rat plasma. The intra- and interday precision in terms of relative standard deviation were <4.98 and 4.84%, resp., at concentration levels of 0.02, 0.20 and 0.80 μg/mL. ADTM’s absolute oral bioavailability value was 30.4% and t1/2 was 34.33 ± 11.51 and 29.94 ± 8.19 min after oral and i.v. administration of 20 mg/kg. In addition, the major metabolites both in vitro and in vivo were 2-hydroxymethy-3,5,6-trimethylpyrazin and DSS. The results indicated that the hydrolysis was the main metabolic pathway of ADTM, and carboxylesterase may play an important role in ADTM’s metabolism The present work provides basic information for ADTM’s further preclin. research and DSS’s chem. structure modification. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Category: pyrazines).
(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine derivatives have antitumor, antibiotic, anticonvulsant, antituberculous and diuretic effects as well as kinase, enzymatic and potent tubulin and FtsZ polymerization inhibitory activities. Pyrazines undergo nearly all of the same reactions as pyrimidines, from nucleophilic substitution (SNAr) to palladium-catalyzed cross coupling reactions.Category: pyrazines