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抑制剂描述:

产品名称:Naloxone HCl

产品别名:见爱必信官网

英文别名:Naloxone HCl

靶点:Others

CAS:357-08-4

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

溶解性:DMSO:73 mg/mL (200.63 mM)
Water:73 mg/mL (200.63 mM)

体外研究:

Naloxone significantly reduces the LPS-induced degeneration of the midbrain neurons. Naloxone inactives stereoisomer (+)-naloxone protected the dopaminergic neurons with equal potency. Naloxone inhibits LPS-induced activation of microglia and release of proinflammatory factors, and inhibition of microglia generation of superoxide free radical best correlated with the neuroprotective effect of naloxone isomers. Naloxone is found to partially inhibit the binding of LPS to cell membranes, whereas it failes to prevent damage to dopaminergic neurons by peroxynitrite, a product of nitric oxide and superoxide. Naloxone (18.0 mg/kg) suppresses water intake when water is presented as the sole source of fluid. Naloxone produces a dose-dependent decrease in ethanol consumption, without altering water intake, when rats are given a free-choice between the ethanol solution and water.

体内研究:Naloxone (10 mg/kg) causes a dose-dependent reduction of break-points and locomotor activity in both the beer and near-beer rats. Naloxone inhibits the LPS-induced activation of microglia and significantly reduces the LPS-induced loss of dopaminergic neurons in the rat substantia nigral. Naloxone abolishes this antinociceptive activity both in the hot-plate test and in the first phase of the formalin test without affecting the serum concentration of paracetamol. Naloxone prevents the increase in 5-HT concentration in the central nervous system and the reduction in 5-HT2 receptors in cortical membranes.

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