Monoamine Receptors in the Regulation of Feeding Behaviour and Energy Balance

: We evaluate the likely utility of drugs that interact, either directly or indirectly, with monoamine binding receptors for the treatment of obesity. We discuss ligands at dopaminergic, adrenergic, serotoninergic and histaminergic receptors and also drugs that either release or inhibit the reuptake of monoamine neurotransmitters. We review evidence from preclinical studies of receptor distribution and function, together with the consequences of gene deletion in transgenic mouse strains and the results from human studies where these are available. In addition we consider the side effect profiles that would be expected of these potential anti-obesity treatments. We conclude that compounds interacting with 5-HT(2C), 5-HT(6) and histamine H(3) receptors may be of particular interest as specific drug development targets for the treatment of appetite disturbance in obesity.