Norfenfluramine is a psychoactive drug

Psychoactive drug

A psychoactive drug, psychopharmaceutical, or psychotropic is a chemical substance that crosses the blood–brain barrier and acts primarily upon the central nervous system where it affects brain function, resulting in changes in perception, mood, consciousness, cognition, and behavior...

 which functions as a serotonin

Serotonin

Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...

 releasing agent

Releasing agent

A releasing agent , or simply releaser, is a drug that induces the release of a neurotransmitter from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitter. Many drugs use neurotransmitter release to exert their psychological and...

 and potent 5HT_2B receptor

5-HT2B receptor

5-hydroxytryptamine receptor 2B, also known as HTR2B, is a 5-HT2 receptor, but also denotes the human gene encoding it.-Function:...

 agonist

Agonist

An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...

. The action of norfenfluramine on 5HT_2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblast

Fibroblast

A fibroblast is a type of cell that synthesizes the extracellular matrix and collagen, the structural framework for animal tissues, and plays a critical role in wound healing...

s on the tricuspid valve

Tricuspid valve

The tricuspid valve, or right atrioventricular valve, is on the right dorsal side of the mammalian heart, between the right atrium and the right ventricle. The normal tricuspid valve usually has three leaflets and three papillary muscles. They are connected to the papillary muscles by the chordae...

, known as cardiac fibrosis

Cardiac fibrosis

Cardiac fibrosis refers to an abnormal thickening of the heart valves due to inappropriate proliferation of cardiac fibroblasts.Fibrocyte cells normally secrete collagen, and function to provide structural support for the heart...

. This side effect led to the withdrawal of fenfluramine

Fenfluramine

Fenfluramine is a drug that was part of the Fen-Phen anti-obesity medication . Fenfluramine was introduced on the U.S. market in 1973. It is the racemic mixture of two enantiomers, dextrofenfluramine and levofenfluramine...

 as an anorectic

Anorectic

An anorectic or anorexic , also known as anorexigenic or appetite suppressant, is a dietary supplement and/or drug which reduces appetite, food consumption, and as a result, causes weight loss to occur.-List of anorectics:Numerous pharmaceutical compounds are marketed as appetite suppressants.The...

 drug worldwide, and to the withdrawal of benfluorex

Benfluorex

Benfluorex is an anorectic and hypolipidemic agent that is structurally related to fenfluramine. Two clinical studies have shown it may improve glycemic control and decrease insulin resistance in people with poorly controlled type 2 diabetes; However Servier is suspected of having marketed Mediator...

 in Europe, as both fenfluramine and benfluorex form norfenfluramine as a metabolite

Metabolite

Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...

.

Norfenfluramine has also been shown to be vasoactive in its own right, causing pulmonary hypertension

Pulmonary hypertension

In medicine, pulmonary hypertension is an increase in blood pressure in the pulmonary artery, pulmonary vein, or pulmonary capillaries, together known as the lung vasculature, leading to shortness of breath, dizziness, fainting, and other symptoms, all of which are exacerbated by exertion...

.

See also

• 3-Fluoroamphetamine
  3-Fluoroamphetamine
  3-Fluoroamphetamine is a stimulant drug from the amphetamine family which acts as a monoamine releaser with similar potency to methamphetamine but more selectivity for dopamine and noradrenaline release over serotonin...
  
  
• 3-Methylamphetamine
  3-Methylamphetamine
  3-Methylamphetamine is a stimulant drug from the amphetamine family. It is self-administered by mice to a similar extent to 4-fluoroamphetamine and has comparable properties as a monoamine releaser, although with a more balanced release of all three monoamines, as opposed to the more...
  
  
• 3-Methoxyamphetamine
  3-Methoxyamphetamine
  meta-Methoxyamphetamine , also known as 3-methoxyamphetamine , is a stimulant drug from the amphetamine family...
  
  
• Substituted amphetamine
  Substituted amphetamine
  Substituted amphetamines are a chemical class of stimulants, entactogens, hallucinogens, and other drugs. They feature a phenethylamine core with a methyl group attached to the alpha carbon resulting in amphetamine, along with additional substitutions...
  
  
• Gepefrine
  Gepefrine
  Gepefrine , also known as α-methyl-​meta-tyramine, is a cardiac stimulant drug.- See also :* 3-Methoxyamphetamine * 3-Methylamphetamine * 3-Fluoroamphetamine...
  
  
• Desmethylcitalopram
  Desmethylcitalopram
  Desmethylcitalopram is an active metabolite of the antidepressant drugs citalopram and escitalopram...
  
  
• Desmethylsertraline
  Desmethylsertraline
  Desmethylsertraline is an active metabolite of the antidepressant drug sertraline. Like sertraline, desmethylsertraline functions as a selective serotonin reuptake inhibitor , and is responsible for some of its parent's therapeutic benefits....
  
  
• Norfluoxetine
  Norfluoxetine
  Seproxetine, also known as -norfluoxetine, is a selective serotonin reuptake inhibitor . It is an active metabolite of fluoxetine. Seproxetine was being investigated by Eli Lilly and Company as an antidepressant but development was never completed and the drug was never marketed.-Synthesis:Fuller,...