Bayer CropScience AG, BCS AG R&D-SMR-PC-PCC C2, Alfred-Nobel-Strasse 50, Building 6510, 40789 Monheim am Rhein, Germany.
Angew Chem Int Ed Engl. 2013 Sep 2;52(36):9464-85. doi: 10.1002/anie.201302550. Epub 2013 Aug 9.
The destruction of crops by invertebrate pests is a major threat against a background of a continuously rising demand in food supply for a growing world population. Therefore, efficient crop protection measures in a vast range of agricultural settings are of utmost importance to guarantee sustainable yields. The discovery of synthetic agonists selectively addressing the nicotinic acetylcholine receptors (nAChRs), located in the central nervous system of insects, for use as insecticides was a major milestone in applied crop protection research. These compounds, as a result of their high target specificity and versatility in application methods, opened a new innovative era in the control of some of the world's most devastating insect pests. These insecticides also contributed massively to extending our knowledge of the biochemistry of insect nicotinic acetylcholine receptors. The global economic success of synthetic nAChR agonists as insecticides renders the nicotinic acetylcholine receptor still one of the most attractive target sites for exploration in insecticide discovery.
在不断增长的世界人口对粮食供应需求不断上升的背景下，无脊椎害虫对作物的破坏是一个主要威胁。因此，在广泛的农业环境中采取有效的作物保护措施对于保证可持续产量至关重要。发现合成激动剂可以选择性地针对位于昆虫中枢神经系统中的烟碱型乙酰胆碱受体（nAChRs），并将其用作杀虫剂，这是应用作物保护研究中的一个重要里程碑。这些化合物由于其高靶标特异性和应用方法的多功能性，开创了控制世界上一些最具破坏性的害虫的创新时代。这些杀虫剂还极大地促进了我们对昆虫烟碱型乙酰胆碱受体生物化学的了解。作为杀虫剂的合成 nAChR 激动剂在全球范围内的经济成功，使得烟碱型乙酰胆碱受体仍然是杀虫剂发现中最具吸引力的目标之一。
