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Prazosin (hydrochloride) | 哌唑嗪盐酸盐
MCE 国际站:Prazosin (hydrochloride)
中文名:哌唑嗪盐酸盐
CAS:19237-84-4
品牌:MedChemExpress (MCE)
存储条件:4°C, sealed storage, away from moisture
生物活性:盐酸哌唑嗪是一种耐受性良好的 CNS 活性 α1-肾上腺素能受体 拮抗剂,可用于研究高血压和酒精使用障碍[1]。 Prazosin hydrochloride 有效抑制去甲肾上腺素 (NE) 刺激的 45Ca 外流,IC50 为 0.15 nM[2]。Prazosin hydrochloride 抑制有机阳离子转运蛋白 OCT-1 和 OCT-3 IC50 分别为 1.8 和 13 μM[3]。
体外:哌唑嗪(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[4]。U251和U87细胞的迁移和侵袭[4].哌唑嗪处理降低了PI3K/AKT/mTOR信号通路组分的蛋白表达。哌唑嗪(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[4]。
体内:外周给药哌唑嗪(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[1]。
热销产品:Bimekizumab | WM-8014 | 5'-Methylthioadenosine | Teriparatide | Prexasertib | p-SCN-Bn-DOTA | Palivizumab | Nicotinamide riboside (chloride) | CCR2 antagonist 1 | PDK4-IN-1 (hydrochloride)
研究领域:GPCR/G Protein | Neuronal Signaling | Autophagy
作用靶点:Adrenergic Receptor | Autophagy
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Dennis D Rasmussen, et al. The alpha1-adrenergic receptor antagonist, prazosin, reduces alcohol drinking in alcohol-preferring (P) rats. Alcohol Clin Exp Res. 2009 Feb;33(2):264-72.
[2]. W S Colucci, et al. Nonlinear relationship between alpha 1-adrenergic receptor occupancy and norepinephrine-stimulated calcium flux in cultured vascular smooth muscle cells.Mol Pharmacol. 1985 May;27(5):517-24.
[3]. Deborah L White, et al. OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.Blood. 2006 Jul 15;108(2):697-704.
[4]. Jing Zhang, et al. Prazosin inhibits the proliferation, migration and invasion, but promotes the apoptosis of U251 and U87 cells via the PI3K/AKT/mTOR signaling pathway. Exp Ther Med. 2020 Aug;20(2):1145-1152.
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