Dexmedetomidine HCl 是一种有效的、选择性的、具有口服活性的 α2 肾上腺素能受体 (α2-adrenoceptor) 激动剂，Ki=1.08 nM。它对 α1 肾上腺素受体显示出 1620 倍的选择性。它具有抗焦虑作用，可用于研究促进安定和缓解疼痛。

Dexmedetomidine hydrochloride is an imidazole derivative that is an agonist of the adrenergic alpha-2 receptor. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.

Conivaptan (0.03, 0.1 and 0.3 mg/kg i.v.) dose-dependently increases urine volume and reduces urine osmolality in both myocardial infarction and sham-operated rats. Conivaptan (0.3 mg/kg i.v.) significantly reduces right ventricular systolic pressure, left ventricular end-diastolic pressure, lung/body weight and right atrial pressure in myocardial infarction rats. Conivaptan (0.3 mg/kg i.v.) significantly increases dP/dt(max)/left ventricular pressure in myocardial infarction rats. [1] Conivaptan produces an acute increase in urine volume (UV), a reduction in osmolality (UOsm) and, at the end of the investigation, cirrhotic rats receiving the V(1a)/V(2)-AVP receptor antagonist does not show hyponatremia or hypoosmolality. Conivaptan also normalizes U(Na)V without affecting creatinine clearance and arterial pressure. [2] Conivaptan (0.01 to 0.1 mg/kg i.v.) exerts a dose-dependent diuretic effect in dogs without an increase in the urinary excretion of electrolytes, inhibits the pressor effect of exogenous vasopressin in a dose-dependent manner (0.003 to 0.1 mg/kg i.v.) and, at the highest dose (0.1 mg/kg i.v.), almost completely blocks vasoconstriction caused by exogenous vasopressin. Conivaptan (0.1 mg/kg i.v.) improves cardiac function, as evidenced by significant increases in left ventricular dP/dtmax, cardiac output and stroke volume, and reduces preload and afterload, as evidenced by significant decreases in left ventricular end-diastolic pressure and total peripheral vascular resistance in dogs with congestive heart failure. [3]

In vitro HDAC assay:HDAC activity is analyzed by using an HDAC assay kit. This assay is based on the ability of DU-145 nuclear extract, which is rich in HDAC activity, to mediate the deacetylation of the biotinylated [3H]-acetyl histone H4 peptide that is bound to streptavidin agarose beads. The release of [3H]-acetate into the supernatant is measured to calculate the HDAC activity. Sodium butyrate (0.25-1 mM) is used as a positive control.

145108-58-3

C13H17ClN2

236.74

(+)-Medetomidine hydrochloride;盐酸右美托咪定;(S)-Medetomidine hydrochloride;Precedex;Dexmedetomidine HCl

DMSO:23.7 mg/mL (100 mM)
H2O:23.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years