Przuntek H, Witteler M, Stasch J P, Neuser D, Kuhn W, Russ H
Arzneimittelforschung. 1985;35(5):787-9.
Tocainide (W-36095, Xylotocan) is a derivative of lidocaine which is applied clinically as a cardiac antiarrhythmic. In addition, it diminishes the severity of symptoms in neurological disorders such as myotonia and paramyotonia and in patients with torticollis spasmodicus it brings about a distinct reduction in the tension of the neck muscles. It was investigated whether in reducing the tonus in torticollis spasmodicus tocainide could be acting on the central nervous system. The binding affinity of the substance to the dopamine, serotonin, opiate, GABA and benzodiazepine receptors was measured without finding any significant affinities. In addition, the effect of tocainide on the concentration of the neurotransmitters norepinephrine (noradrenaline), dopamine, serotonin and histamine were investigated in rat brain, and it was found that tocainide induces a significant increase in dopamine and serotonin concentrations. This lead to the conclusion that, in addition to its antiarrhythmic effects, tocainide acts on the central nervous system.
妥卡尼（W - 36095，Xylotocan）是利多卡因的衍生物，在临床上用作心脏抗心律失常药。此外，它能减轻诸如肌强直和僵人综合征等神经疾病的症状严重程度，对于患有痉挛性斜颈的患者，它能使颈部肌肉张力明显降低。研究了妥卡尼在减轻痉挛性斜颈的肌张力时是否作用于中枢神经系统。测量了该物质与多巴胺、血清素、阿片、γ-氨基丁酸（GABA）和苯二氮䓬受体的结合亲和力，未发现任何显著亲和力。此外，在大鼠脑中研究了妥卡尼对神经递质去甲肾上腺素（去甲肾上腺素）、多巴胺、血清素和组胺浓度的影响，发现妥卡尼可使多巴胺和血清素浓度显著升高。由此得出结论，妥卡尼除了具有抗心律失常作用外，还作用于中枢神经系统。
