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J Labelled Comp Radiopharm
Synthesis and Characterization of Deuterated Detomidine for Use in Equine Medication Regulation. Detomidine, 5-[(2,3-dimethylphenyl)methyl]-1H-imidazole, is a tranquilizer/sedative/analgesic widely used in equine medicine and regulated by several different analyte concentrations of detomidine and its hydroxydetomidine and carboxydetomidine metabolites in plasma and urine. Accurate regulatory quantitation of detomidine at low picogram/mL concentrations requires the availability of a stable isotope internal standard of detomidine; however, to the best of our knowledge, no certified deuterated internal standard of detomidine is commercially available and its synthesis has not been reported. ...
Synthesis and Characterization of 3-Hydroxybupivacaine and Deuterated 3-Hydroxybupivacaine for Use in Equine Medication Regulation. Bupivacaine is a local anesthetic widely used in equine and human medicine. Use of bupivacaine in performance horses is regulated because its ability to block pain means that it can be misused for advantage in performance horses. In racing regulation, bupivacaine is classified by the Association of Racing Commissioners International (ARCI) as a Class 2 Penalty Class A Foreign substance, the detection of which can lead to significant penalties. In horses, bupivacaine is metabolized by Phase-I hydroxylation to yield 3-hydroxybupivacaine, which is then glucuronidated to yield the Phase-II metabol...
