货号 | 5037/50 |
别名 | 5-(Aminomethyl)-1-[(2S)-5,7-difluor |
供应商 | Tocris |
生物活性 | Potent and selective dopamine β-hydroxylase (DBH) inhibitor (IC50 = 9 nM) . Selective for DBH over 12 other enzymes. Decreases noradrenaline and increases dopamine levels in tissues and plasma in hypertensive rats. Prevents progressive left ventricular dysfunction in an in vivo heart failure model. Also potentiates the stimulus effects of cocaine without producing cocaine-like effects in rats. Orally bioavailable. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 331.81 |
分子式 | C14H15F2N3 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Manvichet al (2013) Dopamine β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats. J.Pharmacol.Exp.Ther. 347 564. PMID: 24068832. Sabbahet al (2000) Effects of dopamine β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Circulation 102 1990. PMID: 11034950. Stanleyet al (1997) Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br.J.Pharmacol. 121 1803. PMID: 9283721. |