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    Etomidate (R-16659)
    Etomidate (R-16659)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1285
    CAS #: 33125-97-2Purity ≥98%

    Description: Etomidate (Amidate, Ethomidate, Hypnomidate, R-26490, R26490, Radenarkon), discovered at Janssen Pharmaceutica in 1964, is a GABAA receptor agonist that has been approved for use as a short-acting anaesthetic drug or sedative. Etomidate was approved for the induction of general anaesthesia and sedation for short procedures such as reduction of dislocated joints, tracheal intubation, and cardioversion. It was introduced as an intravenous agent in 1972 in Europe and in 1983 in the US. 

    References: Anesthesiology. 2003 Oct;99(4):889-95; Anesthesiology. 2009 Nov;111(5):1025-35.

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    Molecular Weight (MW)244.29
    FormulaC14H16N2O2
    CAS No.33125-97-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 49 mg/mL (200.6 mM)
    Water: <1 mg/mL 49
    Ethanol: 49 mg/mL (200.6 mM)
    Solubility (In vivo)

    Chemical Name: ethyl 3-[(1R)-1-phenylethyl]imidazole-4-carboxylate

    InChi Key: NPUKDXXFDDZOKR-LLVKDONJSA-N

    InChi Code: InChI=1S/C14H16N2O2/c1-3-18-14(17)13-9-15-10-16(13)11(2)12-7-5-4-6-8-12/h4-11H,3H2,1-2H3/t11-/m1/s1

    SMILES Code: O=C(C1=CN=CN1[[email protected]@H](C2=CC=CC=C2)C)OCC

    SynonymsR 26490, Etomidate, Amidate, Ethomidate, Hypnomidate, R-26490, R26490, Radenarkon


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    In Vitro

    In vitro activity: Etomidate rapidly increases phosphorylation of the extracellular signal-related kinases ERK1/2 in alpha2B-receptor-expressing HEK293 cells. Etomidate, via an increase in alpha5GABAAR activity, completely blocks long-term potentiation and impaired memory performance, and these effects are reversed by pretreatment with L-655,708. Etomidate directly activates GABA(A) receptors found in chromaffin cells thereby elevating [Ca(2+)](i). Etomidate modulates GABA(A) receptor activation by muscimol due to the positive anion equilibrium potential, depolarizes chromaffin cells. Etomidate (3-100 mM) suppresses glutamate uptake in a time- and concentration-dependent manner with a half-maximum effect occurring at 2.4 mM. Etomidate leads to a significant decrease of V(max) whereas the K(m) of the transporter is unaffected.

    In VivoEtomidate results in a transient increase (duration 2.4 min) in arterial blood pressure in wild-type mice (17 mmHg). Etomidate (10(-4) M) also inhibits CH tracheal rings contraction in response to cumulative concentrations of CCh and KCl in chronically hypoxic rats. Etomidate and ketamine attenuates pulmonary vasorelaxation in response to acetylcholine and bradykinin, whereas they has no effect on the response to A23187 in canine pulmonary artery. Etomidate and ketamine further attenuates both L-NAME-resistant and TBA-resistant relaxation in canine pulmonary artery. 
    Animal modelRats
    Formulation & DosageN/A
    References

    Anesthesiology. 2003 Oct;99(4):889-95; Anesthesiology. 2009 Nov;111(5):1025-35; Anesth Analg. 2003 Apr;96(4):1035-41; Anesthesiology. 2001 Apr;94(4):668-77.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Etomidate

    Hypnotic effects of etomidate and thiopental in wild-type (WT), α2A-receptor–deficient (α2A-KO), and α2B-receptor–deficient (α2B-KO) mice. Anesthesiology. 2003 Oct;99(4):889-95.
     

    Etomidate

    Cardiovascular effects of etomidate (Eto) in α2A-receptor–deficient (α2A-KO), and α2AB-receptor–deficient (α2AB-KO) mice. Anesthesiology. 2003 Oct;99(4):889-95.
     
    Etomidate
    Etomidate activates mitogen-activated protein kinase phosphorylation via α2B-receptors. Anesthesiology. 2003 Oct;99(4):889-95.


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