Neuronal Histamine and its Receptors: Implication of the Pharmacological Treatment of Obesity

Obesity is the effect of imbalance between energy intake and expenditure and forms a fundamental basis of the metabolic syndrome. A number of substances implicated in the regulation of energy metabolism represent opportunities for anti-obesity drug development. Neuronal histamine and its receptors have been shown to regulate energy metabolism and are considered as anti-obesity targets. Several histamine receptor subtypes have been identified; of these, histamine H(1) and H(3) receptors (H(1)-R and H(3)-R) have been specifically recognized as mediators of energy intake and expenditure. In addition, several histamine drugs related to H(1)-R and H(3)-R, have been shown to attenuate body weight gain both in rodent and human. These results provide the reagents for histamine receptors biology and may find applications in the treatment of obesity and related metabolic disorders. In this review, the development of agonists and antagonists of histamine receptors are provided.