Etomidate(R-16659)

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Etomidate(R-16659)

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	33125-97-2
规格:	≥98%

包装与价格：

包装	价格(元)
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议
2g	电议

产品介绍

Etomidate (Amidate, Ethomidate, Hypnomidate, R-26490, R26490, Radenarkon), discovered at Janssen Pharmaceutica in 1964, is a GABAA receptor agonist that has been approved for use as a short-acting anaesthetic drug or sedative. Etomidate was approved for the induction of general anaesthesia and sedation for short procedures such as reduction of dislocated joints, tracheal intubation, and cardioversion. It was introduced as an intravenous agent in 1972 in Europe and in 1983 in the US.

理化性质和储存条件

Molecular Weight (MW)	244.29
Formula	C14H16N2O2
CAS No.	33125-97-2
Storage	-20℃ for 3 years in powder form
Storage	-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)	Chemical Name: ethyl 3-[(1R)-1-phenylethyl]imidazole-4-carboxylate InChi Key: NPUKDXXFDDZOKR-LLVKDONJSA-N InChi Code: InChI=1S/C14H16N2O2/c1-3-18-14(17)13-9-15-10-16(13)11(2)12-7-5-4-6-8-12/h4-11H,3H2,1-2H3/t11-/m1/s1 SMILES Code: O=C(C1=CN=CN1[C@@H](C2=CC=CC=C2)C)OCC
Synonyms	R 26490, Etomidate, Amidate, Ethomidate, Hypnomidate, R-26490, R26490, Radenarkon

实验参考方法

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.
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	Rats
Formulation & Dosage	N/A
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.