Cell lines

human embryonic kidney (HEK293) cells (with high expression levels of the cloned murine 2A-adrenoceptor ,α2C-adrenoceptor and α2B -adrenoceptor subtypes)

Preparation method

The solubility of this compound in DMSO is >12.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10μM for 20 min

Applications

In membranes from HEK293 cells transfected with α2-receptors, etomidate inhibited binding of the α2-antagonist, [3H]RX821002, with higher potency from α2B- and α2C-receptors than from α2A-receptors.Etomidate activated mitogen-activated protein kinase phosphorylation via α2B -receptors. In α2B-receptor–expressing HEK293 cells, stimulated with 10μM etomidate for 20 min rapidly increased phosphorylation of the extracellular signal-related kinases ERK1/2.

Animal models

α2Adrenoceptor-deficient Mice, α2Bdrenoceptor-deficient Mice

Dosage form

intraperitoneal injection ,5–50 mg/kg body weight

Application

These results showed that 27% of the mice lost the reflex at 10 mg/kg etomidate and all mice transiently lost the righting reflex at 20mg/kg and higher etomidate doses. After injection of etomidate at 30 mg/kg, the righting reflex disappeared in wild-type and α2 A-deficient mice at similar times after intraperitoneal injection. On intravenous injection of etomidate at 30 mg/kg, wild-type mice showed a rapid and transient hypertensive response that was completely absent in mice lacking α2B-receptors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Paris A, Philipp M, Tonner PH., et al. Activation of alpha 2B-adrenoceptors mediates the cardiovascular effects of etomidate. Anesthesiology. 2003 Oct;99(4):889-95.