Division of Neuroscience, Department of Pharmacology, Shrimati Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur (M.S.), India.
Pharmacol Biochem Behav. 2012 Jan;100(3):398-403. doi: 10.1016/j.pbb.2011.09.006. Epub 2011 Oct 2.
The effect of agmatine in preclinical behavioral tests of schizophrenia has been examined in rodents. Agmatine at the doses of 40 and 80 mg/kg blocked conditioned avoidance responding, attenuated apomorphine induced climbing, diminished amphetamine and ketamine hyperlocomotor activity and augmented plasma prolactin levels. Pretreatment of animals with 20 mg/kg of agmatine potentiated the inhibitory effect of haloperidol (0.1 mg/kg, ip) and olanzepine (0.5 mg/kg, ip) in conditioned avoidance response test and apomorphine induced climbing. Agmatine alone at the doses tested here did not induce any cataleptic behavior in mice. However significant catalepsy was exhibited when agmatine (80 mg/kg, ip) was injected to mice pretreated with 5-HT1A receptor antagonist, WAY100, 635. These results indicate that agmatine via regulation of brain dopaminergic signaling modulates dopamine mediated behaviors. The alteration in the levels of endogenous agmatine may contribute to the genesis of psychosis and development of drugs that enhance endogenous agmatine content may be better therapeutic approach to treat schizophrenia with low incidences of extra pyramidal side effects.
胍丁胺在精神分裂症的临床前行为测试中的作用已在啮齿动物中进行了研究。胍丁胺在 40 和 80mg/kg 的剂量下可阻断条件性回避反应,减弱阿扑吗啡诱导的攀爬,减少安非他命和氯胺酮的过度活动,并增加血浆催乳素水平。用 20mg/kg 的胍丁胺预处理可增强氟哌啶醇(0.1mg/kg,ip)和奥氮平(0.5mg/kg,ip)在条件性回避反应测试和阿扑吗啡诱导的攀爬中的抑制作用。在本试验中测试的剂量下,胍丁胺单独使用不会在小鼠中引起任何僵住行为。然而,当预先用 5-HT1A 受体拮抗剂 WAY100635 处理的小鼠注射 80mg/kg 的胍丁胺时,会出现明显的僵住行为。这些结果表明,胍丁胺通过调节大脑多巴胺能信号来调节多巴胺介导的行为。内源性胍丁胺水平的改变可能与精神病的发生有关,而增强内源性胍丁胺含量的药物可能是治疗精神分裂症的更好方法,因为它的锥体外系副作用发生率较低。