盐酸右美托咪定 T6466

Product Introduction
Bioactivity


英文名: Dexmedetomidine hydrochloride

描述: Dexmedetomidine hydrochloride (Precedex) 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。

激酶实验: 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.

体内活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (232.32 mM)
H2O : 23.7 mg/mL (100 mM)


关键字: inhibit | Inhibitor | adrenoceptor | (+)-Medetomidine | Dexmedetomidine hydrochloride | Dexmedetomidine | analgesia | sedation | Beta Receptor | Adrenergic Receptor | anxiolysis | (S)-Medetomidine | Dexmedetomidine Hydrochloride | Medetomidine Hydrochloride

相关产品: Palatrigine | Napitane | DL-Adrenaline Hydrochloride | (±)-N-Methylcoclaurine | Clorprenaline hydrochloride | ADRA1D receptor antagonist 1 HCl | Rotigotine Hydrochloride | Isoferulic acid | Clonidine | Buflomedil hydrochloride

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library

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