Uses
(+)-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].
Definition
ChEBI: (2S)-1-[3-(trifluoromethyl)phenyl]-2-propanamine is a member of amphetamines.
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].
| Animal Model: | Conscious SHAM and DOCA-salt rats[1].
|
| Dosage: | 1-300 μg/kg |
| Administration: | Intravenous injection (i.v.), given in a cumulative fashion at 6-min intervals. |
| Result: | Induced pressor response in conscious SHAM and DOCA-salt rats. (change in mean arterial blood pressure at 300 μg/kg, mm Hg, SHAM vehicle=36, SHAM ketanserin=7, DOCA=51, DOCA ketanserin=19).
|
IC 50
5-HT
2B Receptor: 11.2 nM (Ki); 5-HT
2A Receptor: 1516 nM (Ki); 5-HT
2C Receptor: 324 nM (Ki)
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. DOI:
10.1124/jpet.106.114017[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. DOI:
10.1007/pl00005260[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. DOI:
10.1111/j.1476-5381.1982.tb09169.x
