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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 GABAA receptors over voltage-gated sodium channels (Nav) and L-type voltage-gated calcium channels (Cav; 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 (Item No. 33154) 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.WARNING This product is not for human or veterinary use. | [References]
[1] S LOWSON C S G J P Gent. Convulsive thresholds in mice during the recovery phase from anaesthesia induced by propofol, thiopentone, methohexitone and etomidate.[J]. British Journal of Pharmacology, 1991, 102 4: 879-882. DOI: 10.1111/j.1476-5381.1991.tb12270.x
[2] R. LINGAMANENI H. C H J. Differential interaction of anaesthetics and antiepileptic drugs with neuronal Na+ channels, Ca2+ channels, and GABAA receptors[J]. British journal of anaesthesia, 2003, 90 2: Pages 199-211. DOI: 10.1093/bja/aeg040
[3] ULRIKE E. HILLE. First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases[J]. ACS Medicinal Chemistry Letters, 2010, 2 1: 2-6. DOI: 10.1021/ml100071j
[4] S W LAMBERTS. Differential effects of the imidazole derivatives etomidate, ketoconazole and miconazole and of metyrapone on the secretion of cortisol and its precursors by human adrenocortical cells.[J]. Journal of Pharmacology and Experimental Therapeutics, 1987, 240 1: 259-264.
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