Etomidate

Catalog No.S1329 Synonyms: R16659

Etomidate Chemical Structure

Molecular Weight(MW): 244.29

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

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Biological Activity

Description Etomidate 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
Synonyms R16659

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02822144 Recruiting Stroke Rennes University Hospital September 29, 2016 Phase 3
NCT02453373 Recruiting Stroke|Brain Ischemia Life Recovery Systems|Tulane University School of Medicine January 25, 2017 --
NCT02500225 Active, not recruiting Anesthesia|ECT Inonu University January 2017 Phase 4
NCT02910206 Not yet recruiting Postoperative Complications Zhihong LU|Fourth Military Medical University September 2016 --
NCT02924090 Recruiting Depression University of Manitoba September 2016 Phase 4
NCT02643381 Recruiting Cardiopulmonary Arrest|Respiratory Arrest University of Texas Southwestern Medical Center June 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID