PMID- 15179446
OWN - NLM
STAT- MEDLINE
DCOM- 20041025
LR  - 20191108
IS  - 0897-5957 (Print)
IS  - 0897-5957 (Linking)
VI  - 22
IP  - 2
DP  - 2004 Summer
TI  - Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a 
      newly identified prostaglandin D2 receptor.
PG  - 71-90
AB  - 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.
FAU - Ishizuka, Toshiaki
AU  - Ishizuka T
AD  - Department of Medical Engineering, National Defense Medical College, Namiki 3-2, 
      Tokorozawa, Saitama 359, Japan. tir2@hotmail.com.
FAU - Matsui, Takemi
AU  - Matsui T
FAU - Okamoto, Yasuhiro
AU  - Okamoto Y
FAU - Ohta, Atsuko
AU  - Ohta A
FAU - Shichijo, Michitaka
AU  - Shichijo M
LA  - eng
PT  - Journal Article
PT  - Review
PL  - United States
TA  - Cardiovasc Drug Rev
JT  - Cardiovascular drug reviews
JID - 9006912
RN  - 0 (Carbazoles)
RN  - 0 (Receptors, Immunologic)
RN  - 0 (Receptors, Prostaglandin)
RN  - 0 (Receptors, Thromboxane A2, Prostaglandin H2)
RN  - 0 (Sulfonamides)
RN  - EC 5.3.99.5 (Thromboxane-A Synthase)
RN  - P1ALI72U6C (ramatroban)
RN  - XZF106QU24 (prostaglandin D2 receptor)
SB  - IM
MH  - Airway Obstruction/drug therapy
MH  - Animals
MH  - Arteriosclerosis/pathology/physiopathology
MH  - Capillary Permeability/drug effects
MH  - Carbazoles/pharmacokinetics/*pharmacology/therapeutic use/toxicity
MH  - Clinical Trials as Topic
MH  - Eosinophils/drug effects/immunology
MH  - Humans
MH  - Nasal Mucosa/blood supply
MH  - Receptors, Immunologic/*antagonists & inhibitors
MH  - Receptors, Prostaglandin/*antagonists & inhibitors
MH  - Receptors, Thromboxane A2, Prostaglandin H2/*antagonists & inhibitors
MH  - Rhinitis, Allergic, Perennial/drug therapy
MH  - Rhinitis, Allergic, Seasonal/drug therapy
MH  - Sulfonamides/pharmacokinetics/*pharmacology/therapeutic use/toxicity
MH  - Thromboxane-A Synthase/*metabolism
MH  - Tunica Intima/drug effects/pathology
RF  - 62
EDAT- 2004/06/05 05:00
MHDA- 2004/10/27 09:00
CRDT- 2004/06/05 05:00
PHST- 2004/06/05 05:00 [pubmed]
PHST- 2004/10/27 09:00 [medline]
PHST- 2004/06/05 05:00 [entrez]
AID - 10.1111/j.1527-3466.2004.tb00132.x [doi]
PST - ppublish
SO  - Cardiovasc Drug Rev. 2004 Summer;22(2):71-90. doi: 
      10.1111/j.1527-3466.2004.tb00132.x.