Neurosyphilis, malaria, and the discovery of antipsychotic agents
Neurosyphilis, malaria, and the discovery of antipsychotic agents
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DOI：
10.1080/10673220802432350
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发表时间：
2008-01-01
影响因子：
3.8
通讯作者：
Baldessarini, Ross J.
中科院分区：
文献类型：
--
作者：
Frankenburg, Frances R.;Baldessarini, Ross J.
四种最致残的人类疾病是梅毒、疟疾、精神分裂症和躁狂抑郁症。这些看似无关的疾病的治疗发展史在几个点上相交。用疟疾诱导发热治疗第三期脑梅毒（全身麻痹）获得诺贝尔奖。尽管合成奎宁（一种有效对抗疟疾的植物产品）的尝试失败了，但这些努力鼓励工业有机化学家合成许多有用的物质，包括染料、抗生素和抗组胺药。苯胺衍生的染料亚甲蓝是一类新的多环化学品吩噻嗪的成员。对吩噻嗪类药物进行改良以寻找抗疟药物的努力也失败了，但却产生了新的止吐镇静抗组胺药物，包括异丙嗪、异丙嗪，最终氯丙嗪成为首个有效治疗精神分裂症和躁狂症的药物。氯丙嗪具有抗精神病和抗躁狂的特性，它彻底改变了精神病的治疗方法。
Four of the most disabling human diseases are syphilis, malaria, schizophrenia, and manic-depressive illness. The history of the development of treatments for these seemingly unrelated disorders intersects at several points. Treatment of tertiary cerebral syphilis (general paresis) by inducing fever with malaria led to a Nobel Prize. Although attempts to synthesize quinine, a plant product effective against malaria, failed, these efforts encouraged industrial organic chemists to synthesize many useful substances, including dyes, antibiotics, and antihistamines. The aniline-derived dye methylene blue was a member of a new class of polycyclic chemicals, the phenothiazines. Efforts to modify phenothiazines to find an antimalarial agent also failed but led to novel antiemetic-sedative antihistamines, including promethazine, promazine, and eventually chlorpromazinethe first effective treatment for schizophrenia and mania. Chlorpromazine has antipsychotic and antimanic properties, and it revolutionized the therapeutics of psychotic illnesses.