Yogeeswari Perumal, Sriram Dharmarajan, Ratan Bal Tanushree, Thirumurugan Rathinasabapathy
Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani 333 031, India.
Nat Prod Res. 2006 May 10;20(5):497-505. doi: 10.1080/14786410600604583.
Epibatidine (EPB) (1), an alkaloid isolated from the skin of the Ecuadorian poison frog, Epipedobates tricolor has attracted attention because of its exceptionally powerful analgesic properties: several hundred times greater than those of morphine, and the fact that it acts at nicotine rather than opiate receptors. Although the substance is toxic, it does serve as a lead compound in the development of drugs for pain relief as well as treatment of disorders whose pathogenesis involves nicotinic receptors. In this article, isolation, synthetic methods, effect on neuronal and neuromuscular nicotinic receptors, therapeutic potential, toxicity, nicotinic pharmacophore structural modifications related issues of 1 are discussed.
埃皮巴蒂啶（EPB）（1）是一种从厄瓜多尔三色箭毒蛙皮肤中分离出的生物碱，因其具有异常强大的镇痛特性而备受关注：其镇痛效果比吗啡强数百倍，且作用于烟碱受体而非阿片受体。尽管该物质有毒，但它确实是开发用于缓解疼痛以及治疗发病机制涉及烟碱受体的疾病的药物的先导化合物。本文讨论了1的分离、合成方法、对神经元和神经肌肉烟碱受体的作用、治疗潜力、毒性以及与烟碱药效团结构修饰相关的问题。
