Etomidate

For research use only.

Catalog No.S1329 Synonyms: R16659

Etomidate Chemical Structure

CAS No. 33125-97-2

Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.

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Biological Activity

Description Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
Targets
GABAA receptor [1]
In vitro

Etomidate rapidly increases phosphorylation of the extracellular signal-related kinases ERK1/2 in alpha2B-receptor-expressing HEK293 cells. [1] 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. [2] 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. [3] 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. [4]

In vivo Etomidate results in a transient increase (duration 2.4 min) in arterial blood pressure in wild-type mice (17 mmHg). [1] Etomidate (10(-4) M) also inhibits CH tracheal rings contraction in response to cumulative concentrations of CCh and KCl in chronically hypoxic rats. [5]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. [6]

Protocol

Solubility (25°C)

In vitro DMSO 49 mg/mL (200.58 mM)
Ethanol 49 mg/mL (200.58 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 244.29
Formula

C14H16N2O2

CAS No. 33125-97-2
Storage powder
in solvent
Synonyms R16659
Smiles CCOC(=O)C1=CN=CN1C(C)C2=CC=CC=C2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03240055 Completed Drug: spinal anesthesia|Other: etomidate Dose-Response Relationship Drug General Hospital of Ningxia Medical University June 1 2017 Not Applicable
NCT02174120 Unknown status Drug: propofol|Drug: etomidate Target Controlled Infusion|General Anesthesia Henan Provincial People''s Hospital October 2014 Phase 4
NCT02208596 Unknown status Drug: pentazocine|Drug: propofol|Drug: Etomidate Induced Abortion|Anesthesia Third Affiliated Hospital of Zhengzhou University September 2014 Phase 4
NCT01792037 Completed Drug: Etomidate|Drug: Midazolam|Drug: methylprednisolone Adrenocortical Deficiency|Hemodynamic Instability Istanbul University December 2012 Phase 4
NCT00862381 Completed Drug: Hydrocortisone|Drug: Placebo Patient Admitted in Reanimation University Hospital Grenoble October 2008 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID