Division of Experimental Medicine, Department of Medicine, Imperial College London, Du Cane Road, London, UK.
Brain Res. 2012 Jun 21;1461:111-8. doi: 10.1016/j.brainres.2012.04.032. Epub 2012 Apr 24.
Buspirone is an anxiolytic drug and is a partial agonist for the serotonin 5-HT(1A) receptors as well as possessing low affinity and is an antagonist for the dopamine D(2) autoreceptors, with some evidence of a weak affinity to 5-HT(2) receptors. The underlying mechanism of action of buspirone is not clear; however it is thought that its main pharmacology is mediated via the 5-HT(1A) receptors. Initially developed for use in the treatment of generalised anxiety disorder, it appears that buspirone may be useful in various other neurological and psychiatric disorders, such as attenuating side effects of Parkinson's disease therapy, ataxia, depression, social phobia, and behaviour disturbances following brain injury, and those accompanying Alzheimer's disease, dementia and attention deficit disorder. Considering the potential of this drug to be included in the management of many conditions, thorough and controlled studies are required to elucidate the exact mechanism of action. This review will consider the evidence so far for both the potential underlying mechanisms and its use in various conditions.
丁螺环酮是一种抗焦虑药物，作为 5-羟色胺 5-HT(1A)受体的部分激动剂，对多巴胺 D2 自身受体具有低亲和力和拮抗剂作用，对 5-HT(2)受体具有一定的弱亲和力。丁螺环酮的作用机制尚不清楚；然而，它的主要药理学作用被认为是通过 5-HT(1A)受体介导的。丁螺环酮最初是为治疗广泛性焦虑症而开发的，它似乎在各种其他神经和精神疾病中也可能有用，例如减轻帕金森病治疗、共济失调、抑郁、社交恐惧症、脑损伤后的行为障碍以及伴随的阿尔茨海默病、痴呆和注意缺陷障碍的副作用。鉴于该药有潜力用于许多疾病的治疗，需要进行彻底和对照的研究以阐明其确切的作用机制。这篇综述将考虑到迄今为止关于其潜在作用机制及其在各种疾病中的应用的证据。
