Etomidate-d5

Etomidate-d₅ is intended for use as an internal standard for the quantification of etomidate by GC- or LC-MS. Etomidate is a general anesthetic.^[1] It selectively binds to GABA_A receptors over voltage-gated sodium channels (Na_v) and L-type voltage-gated calcium channels (Ca_v; IC₅₀s = 15.7, 387, and 950 µM, respectively).^[2] Etomidate also inhibits the cytochrome P450 (CYP) isoforms CYP11B1 and CYP11B2 (IC₅₀s = 0.5 and 0.1 nM, respectively), enzymes involved in cortisol and aldosterone biosynthesis, respectively.^[3] It inhibits the production of deoxycortisol and 17α-hydroxy progesterone induced by adrenocorticotropic hormone (ACTH) in dispersed adrenocortical cells isolated from patients with Cushing’s syndrome.^[4] Etomidate (3 mg/kg) induces anesthesia and increases the minimum convulsive dose of pentylenetetrazole during the recovery period, but also induces myoclonus, in mice.^[1] Formulations containing etomidate have been used as general anesthetics.

References:
[1].Lowson, S., Gent, J.P., and Goodchild, C.S.Convulsive thresholds in mice during the recovery phase from anaesthesia induced by propofol, thiopentone, methohexitone and etomidateBr. J. Pharmacol.102(4)879-882(1991).
[2].Lingamaneni, R., and Hemmings, H.C., Jr.Differential interaction of anaesthetics and antiepileptic drugs with neuronal Na+ channels, Ca2+ channels, and GABAA receptorsBr. J. Anaesth.90(2)199-211(2003).
[3].Hille, U.E., Zimmer, C., Vock, C.A., et al.First selective CYP11B1 inhibitors for the treatment of cortisol-dependent diseasesACS Med. Chem. Lett.2(1)2-6(2010).
[4].Lamberts, S.W., Bons, E.G., Bruining, H.A., et al.Differential effects of the imidazole derivatives etomidate, ketoconazole and miconazole and of metyrapone on the secretion of cortisol and its precursors by human adrenocortical cellsJ. Pharmacol. Exp. Ther.240(1)259-264(1987).