CORE--BIOANALYTICAL CORE

核心--生物分析核心

• 批准号: 6104013
• 负责人: HENRY I YAMAMURA
• 金额: $ 10.45万
• 依托单位: UNIVERSITY OF ARIZONA
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-04-01 至 2000-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6104013
• 关键词: analgesics; analytical chemistry; bioassay; biomedical facility; blood brain barrier; drug screening /evaluation; guinea pigs; laboratory mouse; laboratory rat; membrane permeability; opioid receptor; peptide analog; receptor binding; synthetic peptide; tissue /cell preparation

The Program Project that this Bioanalytical Core Proposal is part of intends to develop new opioid analgesic drugs that will replace existing narcotics. It is anticipated that these new drugs will be as effective as existing opiate drugs but will be safer and have less abuse potential. The Bioanalytical Core Proposal provides essential analytical services to other parts of the associated Program Project responsible for the development of new opioid peptide and peptide-like compounds. These services include measurements of binding afinity at the different opioid receptor types, measurements of potency using isolated tissue assays, determination stability against degradation by tissue, studies of the ability of these compounds to pass membrane barriers and analgestic activity after direct injection into the brain and after systemic injection. The basic information on opioid receptor binding affinity and potency will be obtained for all compounds under development. Compounds selected from these studies will be further tested using the other three approaches. Stability, membrane permeation and analgesic activity studies will identify new compounds most likely to have clinical utility as new opioid drugs.

该生物分析核心提案所属的计划项目 打算开发新的阿片类镇痛药 取代现有的麻醉剂。 预计这些新 药物将与现有阿片类药物一样有效，但会 更安全，滥用可能性更小。 生物分析核心提案提供了必要的分析 为相关计划项目的其他部分提供服务 负责新阿片肽的开发和 肽类化合物。 这些服务包括测量 不同阿片受体类型的结合亲和力， 使用分离的组织测定法测量效力， 测定对组织降解的稳定性，研究 这些化合物通过膜屏障的能力 直接注射到大脑后的镇痛活性 全身注射后。 阿片类药物的基本信息 所有受体结合亲和力和效力都将获得 正在开发的化合物。 选自这些的化合物 将使用其他三种方法进一步测试研究。 稳定性、膜渗透性和镇痛活性研究 将鉴定最有可能具有临床实用性的新化合物 作为新的阿片类药物。