选择性脑穿透 GRPR 拮抗剂在瘙痒症中的作用。-猫眼课题宝

选择性脑穿透 GRPR 拮抗剂在瘙痒症中的作用。

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

项目状态：

已结题

起止时间：

2011-09-30 至 2013-12-30

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

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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.

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Lead candidate identification of LPAR1 antagonists for therapeutic application in NASH

批准号：

10324983
项目类别：
资助金额：

$39.74万
财政年份：

2021
负责人：

Fabio Cohen Tucci
依托单位：

EPIGEN BIOSCIENCES, INC.

Assessment of a selective kinase inhibitor in pre-clinical models of NASH

批准号：

10080619
项目类别：
资助金额：

$37.5万
财政年份：

2020
负责人：

Fabio Cohen Tucci
依托单位：

EPIGEN BIOSCIENCES, INC.

The role of selective brain penetrating GRPR antagonists in pruritis.

批准号：

8236621
项目类别：
资助金额：

$22.44万
财政年份：

2011
负责人：

Fabio Cohen Tucci
依托单位：

EPIGEN BIOSCIENCES, INC.

海外基金