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编 号:F239461
分子式:C19H22ClN5O4
分子量:419.86
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10mM*1mL in DMSO
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100mg
448
In-stock
200mg
720
In-stock
500mg
1440
In-stock
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生物活性:
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.

体内研究:
外周给药 Prazosin hydrochloride (0、0.5、1.0、1.5 或 2.0 mg/kg;ip) 不仅可以抑制中枢 α1 肾上腺素能介导的过度兴奋,还可以抑制应激引起的焦虑。Animal Model:Fifty-five alcohol-naive male rats from the 60th generation of selective breeding for alcohol preference
Dosage:0.5, 1.0, 1.5, or 2.0 mg/kg
Administration:Injected intraperitoneally (IP); 0.5 mg/mL; once a day at 15 min prior to onset of the daily two hour two-bottle choice, alcohol versus water, access period for two consecutive days and then three weeks later for five consecutive days.
Result:Significantly reduced alcohol intake during the initial two daily administrations, and this reduction of alcohol intake was maintained for five consecutive days by daily prazosin treatment in the subsequent more prolonged trial.

体外研究:
Prazosin hydrochloride (0、2.5、5、7.5、10、15、20、30、40 和 50 μM) 有效抑制 U251 和 U87 细胞的增殖。 U251和U87细胞的迁移和侵袭。 Prazosin hydrochloride 处理降低了PI3K/AKT/mTOR信号通路组分的蛋白表达。Prazosin hydrochloride (13.16 和 11.57 μM,用于 U251 和 U87 细胞,48 小时) 降低 P70 和细胞周期蛋白 D1 的表达水平,它们是 PI3K/AKT/mTOR 信号通路的下游靶基因。
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