Metysová J, Metys J, Dlabac A, Kazdová E, Valchár M
Acta Biol Med Ger. 1980;39(6):723-40.
Octoclothepin, 8-chloro-1-(4-methylpiperazino)-10,11-dihydrodibenzo (b,f) thiepin, is a very potent neuroleptic drug with pronounced central antidopaminergic and antiserotonin actions. In most animal experiments, its plharmacological profile resembles that of perphenazine. Octoclothepin reveals an intensive central depressant action in a series of observational and instrumental procedures in rodents. Its active oral doses are within the range of 0.54 to 2.2 mg kg-1 in mice and of 0.1 to 4.8 mg kg-1 in rats. Octoclothepin possesses high cataleptogenic and anti-apomorphine activities in rats; it is able to exert full protection against apomorphine-induced emesis in dogs after the dose of 0.1 mg kg-1 s.c. Octoclothepin reduces some actions and toxicity of d,l-amphetamine and phenmetrazine in rodents. In the rat corpus striatum, octoclothepin in doses of 0.5 and d1.5 mg kg-1 s.c. reduces the DA level and raises the HVA and DOPAC levels significantly. Octoclothepin has antihistamine, antiserotonin and antianaphylactoid actions, it exhibits a high protection against the lethal action of adrenaline and noradrenaline in mice and rats, respectively. Acute toxicological data in mice, rats, rabbits and dogs are given. Clinical antipsychotic effectiveness of octoclothepin has been verified in a large population of psychiatric patients.
八氯噻平，即8-氯-1-(4-甲基哌嗪基)-10,11-二氢二苯并(b,f)硫氮杂卓，是一种非常有效的抗精神病药物，具有显著的中枢抗多巴胺能和抗血清素作用。在大多数动物实验中，其药理学特征与奋乃静相似。八氯噻平在一系列针对啮齿动物的观察性和仪器性实验中显示出强烈的中枢抑制作用。其口服有效剂量在小鼠中为0.54至2.2毫克/千克，在大鼠中为0.1至4.8毫克/千克。八氯噻平在大鼠中具有高度的致僵和抗阿扑吗啡活性；在皮下注射0.1毫克/千克的剂量后，它能够对犬阿扑吗啡诱导的呕吐发挥完全保护作用。八氯噻平可降低啮齿动物中d,l-苯丙胺和苯甲曲秦的一些作用及毒性。在大鼠纹状体中，皮下注射0.5和1.5毫克/千克剂量的八氯噻平可降低多巴胺水平，并显著提高高香草酸和3,4-二羟基苯乙酸水平。八氯噻平具有抗组胺、抗血清素和抗过敏样作用，它分别对小鼠和大鼠中肾上腺素和去甲肾上腺素的致死作用表现出高度保护作用。给出了小鼠、大鼠、兔子和犬的急性毒理学数据。八氯噻平的临床抗精神病有效性已在大量精神科患者中得到验证。
