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中文摘要
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NIMH精神活性药物筛选计划(PDSP)的目的是为科学研究界提供广泛的筛选能力(药理学和功能测定)和受体结合数据,以刺激创新的研究和开发工作,发现和设计用于基础研究,神经成像的新型精神活性化合物,并作为治疗精神疾病的潜在治疗剂。PDSP的活动包括筛选目前使用的药理学工具和治疗剂以描述其活性,筛选具有功能或行为效应的化合物以鉴定其受体靶点,选择性筛选新的潜在研究工具和成像配体,体外功效测试和潜在治疗剂的反筛选,以及筛选具有未知活性的合成和天然产物库。此外,该程序还支持数千种化合物在数百种受体上的亲和常数的大型数据库。这些数据可以被挖掘,为新工具或药物发现项目提供起点,或确定潜在的新干预目标。目前,该项目有超过225种检测方法可用于筛选,包括体外ADME和毒性筛选。
英文摘要
The objective of the NIMH Psychoactive Drug Screening Program (PDSP) is to provide broad screening capabilities (pharmacological and functional assays) and receptor binding data to the scientific research community to stimulate innovative research and development efforts in the discovery and design of novel psychoactive compounds for basic research, neuroimaging, and as potential therapeutic agents in the treatment of psychiatric disorders. Activities of the PDSP include screening currently used pharmacological tools and therapeutics to profile their activity, screening compounds with functional or behavioral effects to identify their receptor targets, selectivity screening of new potential research tools and imaging ligands, in vitro efficacy testing and counter-screening of potential therapeutics, and screens of synthetic and natural product libraries with unknown activity. In addition, the program supports a large database of affinity constants for thousands of compounds at hundreds of receptors. This data can be mined to provide starting points for new tool or drug discovery projects or identify potential new targets for intervention. Currently, the program has over 225 assays available for screening, including in vitro ADME and toxicity screens.
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Mechanistic insights into LSD actions at 5-HT2A serotonin receptors
STRUCTURE AND FUNCTION OF MRG-FAMILY RECEPTORS
STRUCTURE AND FUNCTION OF MRG-FAMILY RECEPTORS
Mechanistic insights into LSD actions at 5-HT2A serotonin receptors
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