Drug Development

药物开发

• 批准号: 8330550
• 负责人: KELVIN W. GEE
• 金额: $ 36.91万
• 依托单位: UNIVERSITY OF COLORADO DENVER
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-09-21 至 2016-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8330550
• 关键词: Animal Model; Antipsychotic Agents; Biological Assay; Clinical Trials; Dopamine D2 Receptor; Drug Formulations; Haloperidol; Human; Instruction; Investigation; Modeling; Neurocognitive Deficit; Nicotinic Receptors; Patients; Persons; Pharmaceutical Preparations; Pharmacotherapy; Phase; Phase II Clinical Trials; Plasma; Rattus; Schizophrenia; Simulate; Smoking Behavior; Symptoms; Urine; Work; alpha-bungarotoxin receptor; behavioral pharmacology; cigarette smoking; cognitive function; design; disability; drug development; improved; pre-clinical; preclinical study; psychosocial; receptor function; research study

UCI-40083, a selective positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptor (alpha7 nAChR), was designed and characterized by the team at UC Irvine. Its synthesis for the clinical trials and pre-clinical experiments in this NCDDDG Project will be peformed by medicinal chemists at Newport Scientific Inc., supervised by our team. We will work with Newport Scientific Inc. to conduct the assays and stability studies necessary for its formulation for human use. We will also work with Newport Scientific Inc. to support the assays in plasma and urine forthe Phase 1 and Phase 2 clinical trials. Because Phase 2 trials will be conducted in persons with schizophrenia who are treated with neurolepfic drugs, many of whom smoke cigarettes, the UC Irvine team will perform preclinical animal model studies to determine the effect of UCI-40083 on cognitive function in rats chronically treated with nicofine (to simulate smoking behavior) and/or haloperidol (to simulate antipsychofic treatment).

UCI-40083，α7 烟碱乙酰胆碱受体的选择性正变构调节剂 (PAM) (alpha7 nAChR)，由加州大学欧文分校的团队设计和表征。其合成用于临床 该 NCDDDG 项目中的试验和临床前实验将由药物化学家在 Newport Scientific Inc.，由我们团队监管。我们将与 Newport Scientific Inc. 合作进行 其配方供人类使用所必需的测定和稳定性研究。我们还将与纽波特合作 Scientific Inc. 支持 1 期和 2 期临床试验的血浆和尿液检测。因为 第二阶段试验将在接受神经安定药物治疗的精神分裂症患者中进行，其中许多 对于吸烟的人，加州大学欧文分校团队将进行临床前动物模型研究，以确定 UCI-40083 对长期接受尼可芬（模拟吸烟）治疗的大鼠认知功能的影响 行为）和/或氟哌啶醇（模拟抗精神病治疗）。