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Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor.
Cardiovasc Drug Rev. 2004 Summer; 22(2):71-90.CD

Abstract

It is known that thromboxane A2 (TXA2) contributes to various diseases such as bronchial asthma, ischemic heart disease, cerebrovascular disorders and allergic rhinitis. A number of TXA2 synthase inhibitors and TXA2 receptor (TP receptor) antagonists have been developed to treat these diseases. Ramatroban (BAY u 3405) was developed as a potent TP receptor antagonist with excellent efficacy against allergic rhinitis in many animal models and patients. Recent studies also revealed that ramatroban can block the newly identified PGD2 receptor, chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). PGD2 induces migration and degranulation of eosinophils through CRTh2 and contributes to late-phase inflammation and cell damage. Accordingly, it was considered that ramatroban suppresses the late-phase inflammation via TP receptor and CRTh2 blockade. In terms of the efficacy on vascular systems, it was revealed that ramatroban can suppress the expression of monocyte chemoattractant protein-1 (MCP-1) and adhesion molecules in endothelial cells and prevent exacerbation of inflammation by blocking these responses. According to our recent studies in hypercholesterolemic rabbits ramatroban prevents macrophage infiltration through MCP-1 downregulation and neointimal formation after balloon injury and attenuates vascular response to acetylcholine. Therefore, ramatroban may be beneficial in the treatment of atherosclerosis.

Authors+Show Affiliations

Department of Medical Engineering, National Defense Medical College, Namiki 3-2, Tokorozawa, Saitama 359, Japan. tir2@hotmail.com.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

15179446

Citation

Ishizuka, Toshiaki, et al. "Ramatroban (BAY U 3405): a Novel Dual Antagonist of TXA2 Receptor and CRTh2, a Newly Identified Prostaglandin D2 Receptor." Cardiovascular Drug Reviews, vol. 22, no. 2, 2004, pp. 71-90.
Ishizuka T, Matsui T, Okamoto Y, et al. Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor. Cardiovasc Drug Rev. 2004;22(2):71-90.
Ishizuka, T., Matsui, T., Okamoto, Y., Ohta, A., & Shichijo, M. (2004). Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor. Cardiovascular Drug Reviews, 22(2), 71-90.
Ishizuka T, et al. Ramatroban (BAY U 3405): a Novel Dual Antagonist of TXA2 Receptor and CRTh2, a Newly Identified Prostaglandin D2 Receptor. Cardiovasc Drug Rev. 2004;22(2):71-90. PubMed PMID: 15179446.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor. AU - Ishizuka,Toshiaki, AU - Matsui,Takemi, AU - Okamoto,Yasuhiro, AU - Ohta,Atsuko, AU - Shichijo,Michitaka, PY - 2004/6/5/pubmed PY - 2004/10/27/medline PY - 2004/6/5/entrez SP - 71 EP - 90 JF - Cardiovascular drug reviews JO - Cardiovasc Drug Rev VL - 22 IS - 2 N2 - It is known that thromboxane A2 (TXA2) contributes to various diseases such as bronchial asthma, ischemic heart disease, cerebrovascular disorders and allergic rhinitis. A number of TXA2 synthase inhibitors and TXA2 receptor (TP receptor) antagonists have been developed to treat these diseases. Ramatroban (BAY u 3405) was developed as a potent TP receptor antagonist with excellent efficacy against allergic rhinitis in many animal models and patients. Recent studies also revealed that ramatroban can block the newly identified PGD2 receptor, chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). PGD2 induces migration and degranulation of eosinophils through CRTh2 and contributes to late-phase inflammation and cell damage. Accordingly, it was considered that ramatroban suppresses the late-phase inflammation via TP receptor and CRTh2 blockade. In terms of the efficacy on vascular systems, it was revealed that ramatroban can suppress the expression of monocyte chemoattractant protein-1 (MCP-1) and adhesion molecules in endothelial cells and prevent exacerbation of inflammation by blocking these responses. According to our recent studies in hypercholesterolemic rabbits ramatroban prevents macrophage infiltration through MCP-1 downregulation and neointimal formation after balloon injury and attenuates vascular response to acetylcholine. Therefore, ramatroban may be beneficial in the treatment of atherosclerosis. SN - 0897-5957 UR - https://www.unboundmedicine.com/medline/citation/15179446/Ramatroban__BAY_u_3405_:_a_novel_dual_antagonist_of_TXA2_receptor_and_CRTh2_a_newly_identified_prostaglandin_D2_receptor_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0897-5957&date=2004&volume=22&issue=2&spage=71 DB - PRIME DP - Unbound Medicine ER -