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更新于：2025-05-07

RP-48740

更新于：2025-05-07

概要

概要

基本信息

药物类型

小分子化药

别名

靶点

PAF receptor

作用方式

拮抗剂

作用机制

PAF receptor拮抗剂(血小板活化因子受体拮抗剂)

治疗领域

免疫系统疾病呼吸系统疾病

在研适应症-

非在研适应症

哮喘

原研机构

Sanofi

在研机构-

非在研机构

Sanofi

权益机构-

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C12H11N3OS

InChIKeyARFOASMERCHFBY-UHFFFAOYSA-N

CAS号93363-11-2

关联

100 项与 RP-48740 相关的临床结果

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100 项与 RP-48740 相关的转化医学

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100 项与 RP-48740 相关的专利（医药）

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项与 RP-48740 相关的文献（医药）

2008-04-01·Journal of Chemical Information and Modeling2区 · 化学

A Comparison of Field-Based Similarity Searching Methods: CatShape, FBSS, and ROCS

2区 · 化学

Article

作者: Bravi, Gianpaolo ; Leach, Andrew R. ; Gillet, Valerie J. ; Whittle, Martin ; Moffat, Kirstin

Three field-based similarity methods are compared in retrospective virtual screening experiments. The methods are the CatShape module of CATALYST, ROCS, and an in-house program developed at the University of Sheffield called FBSS. The programs are used in both rigid and flexible searches carried out in the MDL Drug Data Report. UNITY 2D fingerprints are also used to provide a comparison with a more traditional approach to similarity searching, and similarity based on simple whole-molecule properties is used to provide a baseline for the more sophisticated searches. Overall, UNITY 2D fingerprints and ROCS with the chemical force field option gave comparable performance and were superior to the shape-only 3D methods. When the flexible methods were compared with the rigid methods, it was generally found that the flexible methods gave slightly better results than their respective rigid methods; however, the increased performance did not justify the additional computational cost required.

1996-03-01·British Journal of Pharmacology

Protective effect of platelet activating factor antagonists on cultured endothelial cell lysis induced by elastase or activated neutrophils

Article

作者: Renesto, Patricia ; Chignard, Michel ; Paulin, Denise ; Vicart, Patrick

The mechanism(s) responsible for injury of endothelial cells induced by human leukocyte elastase (HLE) was investigated in an immortalized venous human endothelial cell line (IVEC).

First, the proteinase concentrations and incubation delays necessary to trigger a significant IVEC cytotoxicity were determined by chromium assays. Thus, exposure of IVEC for 6 h to 10 μ ml−1HLE resulted in 22 ± 2.8% lysis and 36.4 ± 5.4% detachment (mean ± s.e. mean;n= 4;P< 0.05).

WEB 2086, a specific platelet‐activating factor (PAF) receptor antagonist, induced a significant concentration‐dependent decrease of such a lysis (39.6 ± 7.7% protection at 100 μn= 4). This potential role for PAF was confirmed with two other antagonists of this lipid mediator, i.e., BN 52021 and RP 48740.

Finally, we demonstrated that pretreatment of IVEC with WEB 2086 protected significantly against cell lysis induced by stimulated human neutrophils, an experimental model in which HLE participates.

1996-01-01·Advances in Experimental Medicine and Biology4区 · 医学

The Role of PAF and the Effect of a Specific PAF Antagonist on Local Tissue PO2 and Neuronal Integrity During and After Photothrombotic Brain Infarction in Unanesthetised Rabbits

4区 · 医学

Article

作者: Vermarien, Herman ; Decuyper, Karin ; Bourgain, Rene ; Van Rossem, Koen

The present study was conducted to evaluate the acute effects of a PAF receptor antagonist (RP 48740) on tissue oxygenation, neuronal function, and morphol. damage during and after photothrombotically induced brain infarction in unanesthetized rabbits.The findings indicate the importance of PAF as key mediator of detrimental vascular and/or functional changes related to brain ischemia.

100 项与 RP-48740 相关的药物交易

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