Medetomidine HCl 是一种 α2 肾上腺素受体激动剂,能够作用于α2和α1肾上腺素受体,其Ki分别为1.08 nM和1750 nM。
产品描述
Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
体外活性
Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors. [1]
体内活性
In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. [2] Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover. [3]
Cas No.
86347-15-1
分子式
C13H17ClN2
分子量
236.74
别名
Domitor;Medetomidine HCl;MPV785;Medetomidine hydrochloride
储存和溶解度
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