PROPERTIES OF KAPPA AND A NOVEL OPIATE RECEPTOR IN BRAIN

KAPPA 的特性和脑中新型阿片受体

• 批准号: 3212335
• 负责人: Bruce Lane Nock
• 金额: $ 16.61万
• 依托单位: WASHINGTON UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1990
• 资助国家: 美国
• 起止时间: 1990-03-01 至 1993-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3212335
• 关键词: G protein; adrenocorticotropic hormone; autoradiography; brain; calcium channel; dynorphins; endorphins; guinea pigs; high performance liquid chromatography; laboratory rat; naltrexone; neurochemistry; neuroendocrine system; neuropeptide receptor; opioid receptor; receptor coupling; receptor sensitivity

Two types of binding sites with high affinities for "k"-type opiate drugs are present in brain. These sites appear to be separate entities since they differ in terms biochemical and pharmacological characteristics and are differentially distributed in brain. One site has a high affinity for dynorphin and, therefore, corresponds to what has traditionally been termed the k receptor. The second site, which we refer to as T2 in the proposal, has opiate receptor characteristics but does not appear to be a k receptor since dynorphin and prodynorphin-related peptides have a low affinity for the site. The T2 site also has characteristics that clearly distinguish it from mu and delta opiate receptors. Thus, it is plausible that the T2 site is a major type of receptor for opiates which, heretofore, has been studied to only a limited extent. The endogenous ligand for T2 might be Beta- endorphin since it has a much higher affinity for the site than other endogenous opioids. The studies in this proposal utilize recently developed drugs and procedures that distinguish between the k and T2 receptor and should contribute important information toward establishing the nature and characteristics of the sites and their biochemical and physiological functions.

两种对“k”型阿片类药物具有高亲和力的结合位点 存在于大脑中。 这些网站似乎是独立的实体，因为 它们在生化和药理学特性方面有所不同， 在大脑中的分布存在差异。 一个网站具有很高的亲和力 强啡肽，因此，对应于传统上称为 k受体。 第二个站点，我们在提案中称为 T2， 具有阿片受体特征，但似乎不是 k 受体 因为强啡肽和前强啡肽相关肽对 该网站。 T2站点还具有明显区分的特征 来自 mu 和 delta 阿片受体。 因此，T2 站点是合理的 是阿片类受体的主要类型，迄今为止已对其进行了研究 仅在有限的程度上。 T2 的内源配体可能是 Beta- 内啡肽，因为它对该位点的亲和力比其他位点高得多 内源性阿片类药物。 本提案中的研究利用了最近 开发了区分 k 和 T2 的药物和程序 受体并应为建立 该地点的性质和特征及其生化和 生理功能。