Hydroxyzine dihydrochloride,2192-20-3

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产品名称：Hydroxyzine dihydrochloride

产品别名：盐酸羟嗪

英文别名：Hydroxyzine dihydrochloride

靶点：Histamine H1 receptor

CAS：2192-20-3

纯度：>98%

外观：白色结晶性粉末

保存方法：-20°C

描述：

Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [³H]pyrilamine/[³H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.

溶解性：Ethanol ：12 mg/mL (26.8 mM)
DMSO ：83 mg/mL (185.3 mM)
Water ：83 mg/mL (185.3 mM)

体外研究：

Hydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE). Hydroxyzine (500 µM) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 µg/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen.

体内研究：Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats.

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