Jørgensen Emilie A, Knigge Ulrich, Warberg Jørgen, Kjaer Andreas
Cluster for Molecular Imaging, University of Copenhagen, Copenhagen, Denmark.
Neuroendocrinology. 2007;86(3):210-4. doi: 10.1159/000108341. Epub 2007 Sep 11.
Energy intake and expenditure is regulated by a complex interplay between peripheral and central factors. An exhaustive list of peptides and neurotransmitters taking part in this complex regulation of body weight exists. Among these is histamine, which acts as a central neurotransmitter. In the present article we review current evidence pointing at an important role of histamine in the regulation of appetite and metabolism. Studies using both knockout mouse models as well as pharmacological studies have revealed that histamine acts as an anorexigenic agent via stimulation of histamine H(1) receptors. One effect of histamine in the regulation of appetite is to act as a mediator of the inhibitory effect of leptin on appetite. It seems that histamine may attenuate and delay the development of leptin resistance in high-fat-diet-induced obesity. Furthermore, histamine may also act to accelerate lipolysis. Based on the current evidence of the involvement of histamine in the regulation of body weight, the histaminergic system is an obvious target for the development of pharmacological agents to control obesity. At present, H(3) receptor antagonists that stimulate the histaminergic system may be the most promising histaminergic drugs for antiobesity therapy.
能量摄入与消耗由外周和中枢因素之间复杂的相互作用所调节。参与体重这一复杂调节过程的肽类和神经递质不胜枚举。其中组胺作为一种中枢神经递质发挥作用。在本文中，我们综述了当前表明组胺在食欲和代谢调节中起重要作用的证据。使用基因敲除小鼠模型以及药理学研究均表明，组胺通过刺激组胺H(1)受体发挥厌食剂的作用。组胺在食欲调节中的一个作用是作为瘦素对食欲抑制作用的介导物。组胺似乎可以减轻和延缓高脂饮食诱导的肥胖中瘦素抵抗的发展。此外，组胺还可能起到加速脂肪分解的作用。基于目前组胺参与体重调节的证据，组胺能系统显然是开发控制肥胖的药物的一个靶点。目前，刺激组胺能系统的H(3)受体拮抗剂可能是最有前景的用于抗肥胖治疗的组胺能药物。
