Serotonin 5-ht2c receptor agonists: potential for the treatment of obesity.

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Miller KJ

Serotonin 5-ht2c receptor agonists: potential for the treatment of obesity.

Mol Interv. 2005 Oct;5(5):282-91.

PubMed ID

16249524 [ View in PubMed

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Abstract

Obesity continues to be a burgeoning health problem worldwide. Before their removal from the market, fenfluramine and the more active enantiomer dexfenfluramine were considered to be among the most effective of weight loss agents. Much of the weight loss produced by fenfluramine was attributed to the direct activation of serotonin 5-HT(2C) receptors in the central nervous system via the desmethyl-metabolite of fenfluramine, norfenfluramine. Norfenfluramine, however, is non-selective, activating additional serotonin receptors, such as 5-HT(2A) and 5-HT(2B), which likely mediated the heart valve hypertrophy seen in many patients. Development of highly selective 5-HT(2C) agonists may recapitulate the clinical anti-obesity properties observed with fenfluramine while avoiding the significant cardiovascular and pulmonary side effects.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Fenfluramine	5-hydroxytryptamine receptor 2C	Protein	Humans	Yes	Agonist	Details