Costa-Campos L, Lara D R, Nunes D S, Elisabetsky E
Depto. de Farmacologia, UFRGS, Porto Alegre, Brazil.
Pharmacol Biochem Behav. 1998 May;60(1):133-41. doi: 10.1016/s0091-3057(97)00594-7.
Although recently developed drugs have brought significant improvement, the treatment of psychotic disorders still presents serious drawbacks. Because inherent complexity and lack of satisfactory understanding of the underlying pathophysiology impose limits for rational drug design, resourceful approaches in the search for antipsychotics are pertinent. This article reports pharmacological properties of alstonine, a heteroyohimbine-type alkaloid, which exhibited an antipsychotic-like profile, inhibiting amphetamine-induced lethality, apomorphine-induced stereotypy, and potentiating barbiturate-induced sleeping time. Atypical features of alstonine were the prevention of haloperidol-induced catalepsy and lack of direct interaction with D1, D2 and 5-HT2A receptors, classically linked to antipsychotic mechanism of action.
尽管最近研发的药物已带来显著改善，但精神障碍的治疗仍存在严重缺陷。由于内在的复杂性以及对潜在病理生理学缺乏令人满意的理解，这对合理的药物设计造成了限制，因此寻找抗精神病药物的巧妙方法很有必要。本文报道了异育亨宾类生物碱阿马碱的药理特性，它呈现出类似抗精神病药物的特征，能抑制苯丙胺诱导的致死性、阿扑吗啡诱导的刻板行为，并延长巴比妥类药物诱导的睡眠时间。阿马碱的非典型特征包括预防氟哌啶醇诱导的僵住症，以及与经典抗精神病作用机制相关的D1、D2和5-HT2A受体缺乏直接相互作用。
