Bioactivity | (+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease[1]. |
Invitro | (+)-Norfenfluramine (1 nM to 100 μM) hydrochloride contracts arteries with a dramatic decrease in threshold (aorta and mesenteric resistance artery) in rats[1].(+)-Norfenfluramine (1 and 10 μM, 3 min) hydrochloride induces contraction in aorta from tissues of normotensive and hypertensive rats[1].(+)-Norfenfluramine (0-10 μM, 3 min) hydrochloride induces 5-HT release from rat hippocampal synaptosomes by Ca2+-dependent way [2]. |
In Vivo | (+)-Norfenfluramine (1-300 μg/kg, i.v.) hydrochloride induces pressor response in conscious SHAM and DOCA-salt rats[1].(+)-Norfenfluramine (2.5 and 5 mg/kg, i.p.) hydrochloride decreases of 5-HT and 5-HIAA levels in telencephalon and brainstem of rats[3]. Animal Model: |
Name | (+)-Norfenfluramine hydrochloride |
CAS | 37936-89-3 |
Formula | C10H13ClF3N |
Molar Mass | 239.67 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [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. [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. |