Lidocaine-d10 is intended for use as an internal standard for the quantification of lidocaine by GC- or LC-MS. Lidocaine is an inhibitor of voltage-gated sodium channels (Navs) and a local anesthetic.1,2,3 It inhibits Nav1.2 (Ki = 11 µM), adult and neonatal Nav1.5 (IC50s = 380.1 and 360 µM, respectively), and Nav1.7 and Nav1.8 channels (IC50s = 450 and 104 µM, respectively) expressed in Xenopus oocytes. Topical administration of lidocaine (1-2%) reduces escape behavior in a rhesus monkey model of noxious electrical cutaneous pain.4 Formulations containing lidocaine have been used as local and regional anesthetics.
1.Ragsdale, D.S., McPhee, J.C., Scheuer, T., et al.Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channelsProc. Natl. Acad. Sci. USA93(17)9270-9275(1996) 2.Fraser, S.P., Onkal, R., Theys, M., et al.Neonatal Nav1.5 channels: Pharmacological distinctiveness of a cancer-related voltage-gated sodium channel splice variantBr. J. Pharmacol.Online ahead of print(2021) 3.Chevrier, P., Vijayaragavan, K., and Chahine, M.Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaineBr. J. Pharmacol.142(3)576-584(2004) 4.Lineberry, C.G., and Kulics, A.T.The effects of diazepam, morphine and lidocaine on nociception in rhesus monkeys: A signal detection analysisJ. Pharmacol. Exp. Ther.205(2)302-310(1978)