For research use only.
Catalog No.S1329 Synonyms: R16659
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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Choose Selective GABA Receptor Inhibitors
|Description||Etomidate (R16659) 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)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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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|
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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