化合物Medetomidine HCl T6579

Product Introduction
Bioactivity


英文名: Medetomidine hydrochloride

描述: Medetomidine hydrochloride (MPV785) 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。

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]

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

溶解度: DMSO : 60 mg/mL (253.44 mM)
H2O : 23.7 mg/mL (100 mM)


关键字: Medetomidine hydrochloride | anxiolysis | inhibit | sedation | Medetomidine | α2-adrenoceptor | peripheral nervous system | analgesia | MPV 785 | central nervous system | Inhibitor | Medetomidine Hydrochloride | muscle relaxation | Beta Receptor | MPV-785 | Adrenergic Receptor

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