37936-89-3

37936-89-3 structure

Name: (+)-Norfenfluramine hydrochloride
Chemical Name: (2S)-1-[3-(trifluoromethyl)phenyl]propan-2-amine,hydrochloride
CAS Number: 37936-89-3
Molecular Formula: C₁₀H₁₃ClF₃N
Molecular Weight: 239.66500
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2017-03-05 04:29:50
Modify Date: 2024-01-05 07:03:40
(+)-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].

Name	(2S)-1-[3-(trifluoromethyl)phenyl]propan-2-amine,hydrochloride

Description	(+)-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].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2B Receptor:11.2 nM (Ki) 5-HT2C Receptor:324 nM (Ki) 5-HT2A Receptor:1516 nM (Ki)
In Vitro	(+)-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: 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).
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. [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.

Molecular Formula	C₁₀H₁₃ClF₃N
Molecular Weight	239.66500
Exact Mass	239.06900
PSA	26.02000
LogP	4.09740
Storage condition	2-8°C

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
RIDADR	NONH for all modes of transport

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