Catalog No.S1329 Synonyms: R16659
Molecular Weight(MW): 244.29
Etomidate is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
Purity & Quality Control
Choose Selective GABA Receptor Inhibitors
|Description||Etomidate is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.|
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 vivo||Etomidate 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. |
-  Paris A, et al. Anesthesiology,?003, 99(4), 889-895.
-  Martin LJ, et al. Anesthesiology,?009, 111(5), 1025-1035.
-  Xie Z, et al. J Physiol,?004, 560(Pt 3), 677-690.?
|In vitro||DMSO||49 mg/mL (200.58 mM)|
|Ethanol||49 mg/mL (200.58 mM)|
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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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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