Obesity is considered one of the risk factors for metabolic disorders. There is increasing evidence that obesity is under control of several cytokines and hormone in the brain. Brain histamine and H3 receptors are important factors for regulating obesity. The results of physiological and pharmacological studies revealed that brain histamine and H3 receptors are involved in the regulation of obesity. In this review, we describe the implication and patent for developing H3 receptor antagonists and their therapeutic potential of obesity.