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The role of selective brain penetrating GRPR antagonists in pruritis.

选择性脑穿透 GRPR 拮抗剂在瘙痒症中的作用。

基本信息

批准号：
8338820
负责人：
Fabio Cohen Tucci
金额：
$ 18.4万
依托单位：
EPIGEN BIOSCIENCES, INC.
依托单位国家：
美国
项目类别：
财政年份：
2011
资助国家：
美国
起止时间：
2011-09-30 至 2013-12-30
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8338820
关键词：
Ablation Address Affinity Animal Model Animals Antipruritics Behavior Binding Biological Assay Bombesin Receptor Brain CD80 gene Cell Membrane Permeability Chemicals Chronic Clinical Computer Simulation Data Dorsal Dose Drug Delivery Systems Etiology GRP gene Goals Histamine Human Cloning Humulus In Vitro Knock-out Laboratories Lead Ligands Literature Mediating Mediation Medical Methodology Modality Modeling Oral Administration Penetration Pharmaceutical Chemistry Pharmaceutical Preparations Pharmacology Plasma Play Preclinical Drug Evaluation Property Pruritus Reporting Research Research Design Research Methodology Rodent Model Role Screening procedure Series Spinal Cord Structure-Activity Relationship System Technology Testing Validation Work base behavior measurement design drug development effective therapy high throughput technology in vivo innovation interest meetings novel pharmacophore pre-clinical receptor response scaffold small molecule therapeutic development therapeutic target tool

项目摘要

DESCRIPTION (provided by applicant): The goal is to discover novel selective CNS penetrant antagonists of the GRP receptor (GRPR) as probes to validate a new target implicated in pruritic responses. In this work, new compounds will be identified utilizing our assay cascade incorporating in vitro receptor pharmacology and novel in vivo screening tools for evaluating pruritic behavior. Candidate ligands will be designed and synthesized using a series of recognized approaches in medicinal chemistry to have a high likelihood of CNS penetration. Compounds that meet our in vitro criteria will be assessed in a series of pre-clinical pruritis models to evaluate the role of this receptor in pruritis. This work will determine the involvement of GRPR in the pruritic response and determine its utility as a potential drug target.

描述（由申请人提供）：目的是发现新型选择性GRP受体（GRPR）CNS渗透拮抗剂作为探针，以验证与炎症反应有关的新靶点。在这项工作中，将确定新的化合物，利用我们的试验级联结合体外受体药理学和新的体内筛选工具，以评估药理学行为。候选配体将使用药物化学中一系列公认的方法设计和合成，以具有较高的CNS渗透可能性。将在一系列临床前尿道炎模型中评估符合我们的体外标准的化合物，以评价该受体在尿道炎中的作用。这项工作将确定GRPR参与炎症反应，并确定其作为潜在药物靶点的效用。