product name Etomidate
Description: Etomidate (also known as R16659) is a GABAA receptor agonist that is used as a short-acting anaesthetic agent or sedative. Etomidate is used for the induction of general anaesthesia and sedation for short procedures such as reduction of dislocated joints, tracheal intubation, and cardioversion. It was discovered at Janssen Pharmaceutica in 1964 and 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.
244.29
Formula
C14H16N2O2
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)
Synonyms
R16659
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19421783
| 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| 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. |
