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MedChemExpress - Model (+)-Norfenfluramine -19036-73-8
(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease[1].MCE products for research use only. We do not sell to patients.
(+)-Norfenfluramine
MCE China：(+)-Norfenfluramine
Brand：MedChemExpress (MCE)
Cat. No.HY-W131725
CAS：19036-73-8
Purity：98.79%
Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease.
In Vitro：(+)-Norfenfluramine (1 nM to 100 μM) contracts arteries with a dramatic decrease in threshold (aorta and mesenteric resistance artery) in rats[1]. (+)-Norfenfluramine (1 and 10 μM, 3 min) induces contraction in aorta from tissues of normotensive and hypertensive rats[1]. (+)-Norfenfluramine (0-10 μM, 3 min) induces 5-HT release from rat hippocampal synaptosomes by Ca2+-dependent way [2].
In Vivo：(+)-Norfenfluramine (1-300 μg/kg, i.v.) induces pressor response in conscious SHAM and DOCA-salt rats[1]. (+)-Norfenfluramine (2.5 and 5 mg/kg, i.p.) decreases of 5-HT and 5-HIAA levels in telencephalon and brainstem of rats[3].
IC50 & Target：5-HT2B Receptor 11.2 nM (Ki) 5-HT2A Receptor 1516 nM (Ki) 5-HT2C Receptor 324 nM (Ki)
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References：
[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. [Content Brief]
[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. [Content Brief]
[3]. R Invernizzi, et al. Is receptor activation involved in the mechanism by which (+)-fenfluramine and (+)-norfenfluramine deplete 5-hydroxytryptamine in the rat brain? Br J Pharmacol. 1982 Mar;75(3):525-30. [Content Brief]
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