INSECTICIDE ACTIONS ON NICOTINIC ACETYLCHOLINE RECEPTORS

对烟碱乙酰胆碱受体的杀虫作用

• 批准号: 8072489
• 负责人: GUSTAV AKK
• 金额: $ 0.96万
• 依托单位: WASHINGTON UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-02-10 至 2010-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8072489
• 关键词: Abnormal coordination; Exposure to; Goals; Human; Insecta; Insecticides; Learning; Mammals; Muscle; Neurons; Nicotine; Nicotinic Agonists; Nicotinic Receptors; Property; Receptor Activation; Recombinants; Research; Symptoms; Testing; Toxic effect; Tremor; Whole-Cell Recordings; Work; base; design; imidacloprid; insight; natural hypothermia; novel; patch clamp; public health relevance; receptor; receptor function; research study; response

DESCRIPTION (provided by applicant): The nicotinic acetylcholine receptor (nAChR) is the target of synthetic, nicotine-based insecticides, called neonicotinoids. The proposed work will examine in detail the interactions of two selected neonicotinoids, imidacloprid and clothianidin, with human muscle (a¿de) and neuronal-type (a4¿2) nAChR. There are two aims. The first aim is to establish the properties of activation and modulation by imidacloprid and clothianidin of the muscle-type nAChR. The second aim is to determine the mechanisms of neuronal-type nAChR modulation by imidacloprid and clothianidin. The results will help to better define the mechanisms of insecticide toxicity, and may be useful in learning how to provide protection from neonicotinoids, as well as provide insights into designing novel, more highly selective neonicotinoids. PUBLIC HEALTH RELEVANCE: Neonicotinoids are synthetic, nicotine-based compounds used as the active ingredients in many widely used insecticides. In mammals, exposure to neonicotinoids can result in tremors and lack of coordination. The nicotinic acetylcholine receptor is the major target of neonicotinoids in mammals. The proposed work will examine the mechanisms of action of two selected neonicotinoids, imidacloprid and clothianidin, on the nAChR.

描述（由应用提供）：烟碱乙酰胆碱受体（NACHR）是合成，基于尼古丁的杀虫剂的靶标，称为新烟碱类药物。拟议的工作将详细研究两种选择的新烟碱类药物，即伊idacloprid和Clothianidin与人类肌肉（A€）和神经元型（A4¿2）NACHR的相互作用。有两个目标。第一个目的是建立肌肉型NACHR的咪二藻醇和dopterianidin的激活和调节的特性。第二个目的是确定咪二藻醇和dopterianidin的神经元型NACHR调节的机制。结果将有助于更好地定义杀虫剂毒性的机制，并且可能有助于学习如何提供新烟碱素的保护，并为设计新颖，更具选择性的新烟碱类动物提供见解。 公共卫生相关性：新烟素是合成的，基于尼古丁的化合物，用作许多广泛使用杀虫剂的活性剂。在哺乳动物中，接触新烟碱可能会导致震颤和缺乏协调性。烟素是哺乳动物中新烟碱类动物的主要靶标。拟议的工作将检查NACHR上两个选定的新烟碱类动物（Imidacloprid和Clothianidin）的作用机理。