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Synthesis and Characterization of 3-Hydroxybupivacaine and Deuterated 3-Hydroxybupivacaine for Use in Equine Medication Regulation.
Journal of labelled compounds & radiopharmaceuticals    March 4, 2025   Volume 68, Issue 3 e4132 doi: 10.1002/jlcr.4132
Arojojoye AS, Holmes J, Buchart MP, Awuah SG, Eisenberg R, Fenger CK, Maylin GA, Tobin T.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...