Mahmood D, Khanam R, Pillai K K, Akhtar M
Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi, India.
Arzneimittelforschung. 2012 May;62(5):222-9. doi: 10.1055/s-0031-1301326. Epub 2012 Feb 13.
Schizophrenia (SCZ) is a debilitating disorder afflicting around 1% of the world population. Recent literature reveals oxidative injuries contribute enormously to the pathophysiology of SCZ alongside other psychopathological disturbances. Histamine H3R-antagonists have shown dual mechanism of action in experimental models of SCZ. Firstly it prevents oxidative stress and secondly alleviates schizophrenic symptoms, particularly the negative symptoms and cognitive deficits. In the present study, histamine H3R-antagonists used were ciproxifan (3.0 mg/kg, ip) and clobenpropit (15 mg/kg, ip) markedly controlled the elevated levels of various oxidative stress markers, for example, thiobarbituric acid reactive substance (TBARS), glutathione (GSH), superoxide dismutase, catalase, etc., as a result of augmented oxidative stress in the experimental models of SCZ such as amphetamine (0.5 mg/kg, sc) and dizocilpine (MK-801) (0.2 mg/kg, ip) induced locomotor hyperactivity, apomorphine (1.5 mg/kg, sc) induced climbing behavior and haloperidol (2.0 mg/kg, po) induced catalepsy. The results of the present study revealed that H3R-antagonists possess antioxidant activity and could serve with dual mechanism by supplementing antioxidant needs of SCZ and at the same time controlling symptoms of SCZ.
精神分裂症(SCZ)是一种使人衰弱的疾病,影响着全球约1%的人口。最近的文献表明,氧化损伤在SCZ的病理生理学中 alongside 其他精神病理障碍起着巨大作用。组胺H3R拮抗剂在SCZ的实验模型中显示出双重作用机制。首先,它可预防氧化应激,其次可减轻精神分裂症症状,尤其是阴性症状和认知缺陷。在本研究中,所使用的组胺H3R拮抗剂西普噻吩(3.0毫克/千克,腹腔注射)和氯苯丙哌嗪(15毫克/千克,腹腔注射)显著控制了各种氧化应激标志物(例如硫代巴比妥酸反应性物质(TBARS)、谷胱甘肽(GSH)、超氧化物歧化酶、过氧化氢酶等)的升高水平,这些标志物是由于在SCZ实验模型(如苯丙胺(0.5毫克/千克,皮下注射)和地佐环平(MK-801)(0.2毫克/千克,腹腔注射)诱导的运动亢进、阿扑吗啡(1.5毫克/千克,皮下注射)诱导的攀爬行为和氟哌啶醇(2.0毫克/千克,口服)诱导的僵住症)中氧化应激增强所致。本研究结果表明,H3R拮抗剂具有抗氧化活性,可通过满足SCZ的抗氧化需求并同时控制SCZ症状,以双重机制发挥作用。