Etomidate Inhibitor CAS No. 33125-97-2

Cat. No.	Name	Size	Price
KI0964	Etomidate	10 mg	$112
	Etomidate	25 mg	$240
	Etomidate	50 mg	$432

Chemical Characteristic

Product Name	Etomidate
Synonyms	Amidate
CAS No.	33125-97-2
Molecular Weight	244.29
Formula	C₁₄H₁₆N₂O₂
Chemical Structure

Biological activities

Etomidate is a GABAA receptors agonist. Etomidate is a unique drug used for induction of general anesthesia and sedation. Racemic etomidate in rats has lethality at about 12 times effective hypnotic dose (LD50/ED50閳?2), in comparison to barbiturates with LD50/ED50 ratios (therapeutic indices) of 3閳?.^[1] Etomidate differentially inhibits steady-state and peak potassium current with IC50-values of 170 µM for peak current suppression and 120 µM for steady-state current respectively.^[2] Etomidate has a pKa of 4.2 and is very hydrophobic at physiologic pH. In vivo, etomidate impaires contextual fear conditioning with an ED50 dose of 11 mg after intraperitoneal injection in mice.^[3] Etomidate augments GABA-gated chloride currents (indirect action) and, at higher concentrations, evokes chloride currents in the absence of GABA (direct action).^[4]

Protocols

In vivo: Etomidate is dissolved in propylene glycol.^[5]

References

[1] GODEFROI EF, et al. DL-1-(1-arylalkyl)imidazole-5-carboxylate esters. a novel type of hypnotic agents. J Med Chem. 1965, 8: 220-223. 閵嗏偓閵嗏偓 [2] Friederich P, et al. Etomidate inhibits neuronal potassium channels in humans. Anaesthesist. 1997, 46(5): 434-436. 閵嗏偓閵嗏偓 [3] Benkwitz C, et al. Determination of the EC50 amnesic concentration of etomidate and its diffusion profile in brain tissue: implications for in vitro studies. Anesthesiology. 2007, 106(1): 114-123. 閵嗏偓閵嗏偓 [4] Moody EJ, et al. Distinct structural requirements for the direct and indirect actions of the anaesthetic etomidate at GABA(A) receptors. Toxicol Lett. 1998, 100-101: 209-215. 閵嗏偓閵嗏偓 [5] Clarke RS, et al. Adverse effects of intravenously administered drugs used in anaesthetic practice. Drugs. 1981, 22(1): 26-41. 閵嗏偓閵嗏偓

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