(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT 2B receptor agonist (K i : 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease.
性状
Solid
IC50 & Target[1][2]
5-HT2B Receptor 11.2 nM (Ki) 5-HT2C Receptor
体外研究(In Vitro)
(+)-Norfenfluramine (1 nM to 100 μM) hydrochloride contracts arteries with a dramatic decrease in threshold (aorta and mesenteric resistance artery) in rats.(+)-Norfenfluramine (1 and 10 μM, 3 min) hydrochloride induces contraction in aorta from tissues of normotensive and hypertensive rats.(+)-Norfenfluramine (0-10 μM, 3 min) hydrochloride induces 5-HT release from rat hippocampal synaptosomes by Ca-dependent way . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(+)-Norfenfluramine (1-300 μg/kg, i.v.) hydrochloride induces pressor response in conscious SHAM and DOCA-salt rats.
(+)-Norfenfluramine (2.5 and 5 mg/kg, i.p.) hydrochloride decreases of 5-HT and 5-HIAA levels in telencephalon and brainstem of rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Wei Ni, et al. The 5-hydroxytryptamine2A receptor is involved in (+)-norfenfluramine-induced arterial contraction and blood pressure increase in deoxycorticosterone acetate-salt hypertension. J Pharmacol Exp Ther. 2007 May;321(2):485-91. [2]. M Gobbi, et al. In vitro studies on the mechanism by which (+)-norfenfluramine induces serotonin and dopamine release from the vesicular storage pool. Naunyn Schmiedebergs Arch Pharmacol. 1998 Sep;358(3):323-7.
溶解度数据
In Vitro: H2O : 18.75 mg/mL (78.23 mM; ultrasonic and warming and heat to 60°C)配制储备液