Norfenfluramine (original) (raw)
Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist.
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dbo:abstract | La norfenfluramine (3-trifluorométhylamphétamine) est une substance anorexigène appartenant au groupe des amphétamines. Ce serait aussi un psychotrope stimulant, en raison de propriétés sérotoninergiques : * stimulation de la libération de sérotonine ; * puissante activité agoniste vis-à-vis des récepteurs 5HT2B, mais cette activité est considérée comme négligeable (voir ci-dessous).La norfenfluramine n'a pas été commercialisée ; c'est un métabolite actif de trois médicaments, la fenfluramine (Pondéral), la dexfenfluramine (Isoméride) (sous forme S) et le benfluorex (Mediator), retirés du marché. (fr) Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist. (en) ノルフェンフルラミン(Norfenfluramine)または3-トリフルオロメチルアンフェタミンはアンフェタミン系の薬剤で、セロトニン及びノルエピネフリンの、また、、の強いアゴニストである。心臓弁の5-HT2B受容体におけるノルフェンフルラミンの作用は、三尖弁の線維芽細胞が増殖後に特徴的なパターンの心不全を引き起こす。この副作用のため、世界中でとして用いられていたノルフェンフルラミンは市場から撤退した。また、ベンフルオレクスとはノルフェンフルラミンのであることから、ヨーロッパで用いられていたベンフルオレクスも用いられなくなった。ヒトののアゴニストとして作用する。 (ja) Norfenfluramina, também conhecida como 3-Trifluorometilanfetamina, é uma droga nunca comercializada da classe química das anfetaminas que atua como agente liberador de serotonina e noradrenalina, especialmente como agonista potente dos receptores 5-HT 2A, 5-HT2B e 5-HT2C. A ação da norfenfluramina nos receptores 5-HT2B nas válvulas cardíacas provoca o desenvolvimento característico de insuficiência cardíaca após a proliferação de fibroblastos na válvula tricúspide, de modo que provoca fibrose cardíaca. Esse efeito colateral levou à retirada da fenfluramina como agente anorexígeno em todo o mundo e à retirada do benfluorex [en] na Europa, pois tanto a fenfluramina quanto o benfluorex possuem a norfenfluramina como metabólito ativo. Também é um agonista do receptor associado a aminas traço do tipo 1 (TAAR1 [en]). (pt) |
dbo:alternativeName | 3-Trifluoromethylamphetamine (en) |
dbo:iupacName | 1-[3-(Trifluoromethyl)phenyl]propan-2-amine (en) |
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dbp:imagealt | Ball-and-stick model of the norfenfluramine molecule (en) |
dbp:imagefile | Norfenfluramine molecule ball from xtal.png (en) Norfenfluramine.png (en) |
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rdfs:comment | Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist. (en) ノルフェンフルラミン(Norfenfluramine)または3-トリフルオロメチルアンフェタミンはアンフェタミン系の薬剤で、セロトニン及びノルエピネフリンの、また、、の強いアゴニストである。心臓弁の5-HT2B受容体におけるノルフェンフルラミンの作用は、三尖弁の線維芽細胞が増殖後に特徴的なパターンの心不全を引き起こす。この副作用のため、世界中でとして用いられていたノルフェンフルラミンは市場から撤退した。また、ベンフルオレクスとはノルフェンフルラミンのであることから、ヨーロッパで用いられていたベンフルオレクスも用いられなくなった。ヒトののアゴニストとして作用する。 (ja) La norfenfluramine (3-trifluorométhylamphétamine) est une substance anorexigène appartenant au groupe des amphétamines. Ce serait aussi un psychotrope stimulant, en raison de propriétés sérotoninergiques : * stimulation de la libération de sérotonine ; * puissante activité agoniste vis-à-vis des récepteurs 5HT2B, (fr) Norfenfluramina, também conhecida como 3-Trifluorometilanfetamina, é uma droga nunca comercializada da classe química das anfetaminas que atua como agente liberador de serotonina e noradrenalina, especialmente como agonista potente dos receptores 5-HT 2A, 5-HT2B e 5-HT2C. A ação da norfenfluramina nos receptores 5-HT2B nas válvulas cardíacas provoca o desenvolvimento característico de insuficiência cardíaca após a proliferação de fibroblastos na válvula tricúspide, de modo que provoca fibrose cardíaca. Esse efeito colateral levou à retirada da fenfluramina como agente anorexígeno em todo o mundo e à retirada do benfluorex [en] na Europa, pois tanto a fenfluramina quanto o benfluorex possuem a norfenfluramina como metabólito ativo. Também é um agonista do receptor associado a aminas traço d (pt) |
rdfs:label | Norfenfluramine (fr) ノルフェンフルラミン (ja) Norfenfluramine (en) Norfenfluramina (pt) |
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