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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/10/16 21:48:28」(JST)

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Ramatroban (INN) is a thromboxane receptor antagonist.^[1]

It is also a CRTH2 antagonist.^[2]

It is indicated for the treatment of coronary artery disease.^[3] It has also been used for the treatment of asthma.^[4]

It was developed by the German pharmaceutical company Bayer AG and is co-marketed in Japan by Bayer and Nippon Shinyaku Co. Ltd. under the tradename Baynas.

References

^ Sugimoto H, Shichijo M, Iino T et al. (April 2003). "An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro". J. Pharmacol. Exp. Ther. 305 (1): 347–52. doi:10.1124/jpet.102.046748. PMID 12649388.
^ Royer JF, Schratl P, Carrillo JJ et al. (September 2008). "A novel antagonist of prostaglandin D2 blocks the locomotion of eosinophils and basophils". Eur. J. Clin. Invest. 38 (9): 663–71. doi:10.1111/j.1365-2362.2008.01989.x. PMID 18837743.
^ Fiedler VB, Seuter F, Perzborn E (December 1990). "Effects of the novel thromboxane antagonist Bay U 3405 on experimental coronary artery disease". Stroke 21 (12 Suppl): IV149–51. PMID 2260140.
^ Endo S, Akiyama K (November 1996). "[Thromboxane A2 receptor antagonist in asthma therapy]". Nippon Rinsho (in Japanese) 54 (11): 3045–8. PMID 8950952.

External links

(Japanese) Baynas

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English Journal

Central CRTH2, a second prostaglandin D2 receptor, mediates emotional impairment in the lipopolysaccharide and tumor-induced sickness behavior model.

Haba R1, Shintani N, Onaka Y, Kanoh T, Wang H, Takenaga R, Hayata A, Hirai H, Nagata KY, Nakamura M, Kasai A, Hashimoto R, Nagayasu K, Nakazawa T, Hashimoto H, Baba A.
The Journal of neuroscience : the official journal of the Society for Neuroscience.J Neurosci.2014 Feb 12;34(7):2514-23. doi: 10.1523/JNEUROSCI.1407-13.2014.
Chemoattractant receptor-homologous molecule expressed on T helper type 2 cells (CRTH2) is a second prostaglandin D2 receptor involved in mediating the allergic response; however, its central function is not yet known. Here, we demonstrate that central CRTH2 mediates emotional impairment. Lipopolysa
PMID 24523542

Inverse agonism of SQ 29,548 and Ramatroban on Thromboxane A2 receptor.

Chakraborty R1, Bhullar RP2, Dakshinamurti S3, Hwa J4, Chelikani P5.
PloS one.PLoS One.2014 Jan 23;9(1):e85937. doi: 10.1371/journal.pone.0085937. eCollection 2014.
G protein-coupled receptors (GPCRs) show some level of basal activity even in the absence of an agonist, a phenomenon referred to as constitutive activity. Such constitutive activity in GPCRs is known to have important pathophysiological roles in human disease. The thromboxane A2 receptor (TP) is a
PMID 24465800

Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of "chemoattractant receptor homologous molecule expressed on Th2 cells" (CRTH2).

Tasaki M1, Kobayashi M, Tenda Y, Tsujimoto S, Nakazato S, Numazaki M, Hirano Y, Matsuda H, Terasaka T, Miyao Y, Shimizu Y, Hirayama Y.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2013 Jun 14;49(3):434-40. doi: 10.1016/j.ejps.2013.04.017. Epub 2013 Apr 24.
Chemoattractant receptor homologous molecule expressed on T helper type 2 cells (CRTH2) is a PGD2 receptor found on eosinophils, basophils, and Th2 type T cells which exhibits chemotaxis and functions in activation cascades. However, while a number of CRTH2 antagonists, including ramatroban, are kno
PMID 23624353

Japanese Journal

Prophylactic Effects of the Histamine H1 Receptor Antagonist Epinastine and the Dual Thromboxane A2 Receptor and Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells Antagonist Ramatroban on Allergic Rhinitis Model in Mice

Biological and Pharmaceutical Bulletin 34(4), 507-510, 2011
NAID 130000657839

ラマトロバンと抗ヒスタミン薬の併用による初期療法と飛散後治療の比較

耳鼻咽喉科臨床 99(11), 967-977, 2006-11-01
NAID 10018304739

スギ花粉症患者に対するラマトロバンの安全性

アレルギ-・免疫 13(10), 1458-1464, 2006-10
NAID 40007471342

Related Pictures

★リンクテーブル★

リンク元

「ラマトロバン」

Ramatroban
Systematic (IUPAC) name
	3-((3R)-3-{[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazol-9-yl)propanoic acid
Clinical data
Legal status	℞ Prescription only;
Routes	Oral
Identifiers
CAS number	116649-85-5
ATC code	None
PubChem	CID 123879
IUPHAR ligand	1910
ChemSpider	110413
UNII	P1ALI72U6C
ChEMBL	CHEMBL361812
Chemical data
Formula	C21H21FN2O4S
Mol. mass	416.46 g/mol
	SMILES C1CC2=C(CC1NS(=O)(=O)C3=CC=C(C=C3)F)C4=CC=CC=C4N2CCC(=O)O;
	InChI InChI=1S/C21H21FN2O4S/c22-14-5-8-16(9-6-14)29(27,28)23-15-7-10-20-18(13-15)17-3-1-2-4-19(17)24(20)12-11-21(25)26/h1-6,8-9,15,23H,7,10-13H2,(H,25,26)/t15-/m1/s1; Key:LDXDSHIEDAPSSA-OAHLLOKOSA-N ;

　　[★]

英: ramatroban
商: バイナス

[pmid12649388-1] Sugimoto H, Shichijo M, Iino T et al. (April 2003). "An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro". J. Pharmacol. Exp. Ther. 305 (1): 347–52. doi:10.1124/jpet.102.046748. PMID 12649388.

[pmid18837743-2] Royer JF, Schratl P, Carrillo JJ et al. (September 2008). "A novel antagonist of prostaglandin D2 blocks the locomotion of eosinophils and basophils". Eur. J. Clin. Invest. 38 (9): 663–71. doi:10.1111/j.1365-2362.2008.01989.x. PMID 18837743.

[pmid2260140-3] Fiedler VB, Seuter F, Perzborn E (December 1990). "Effects of the novel thromboxane antagonist Bay U 3405 on experimental coronary artery disease". Stroke 21 (12 Suppl): IV149–51. PMID 2260140.

[pmid8950952-4] Endo S, Akiyama K (November 1996). "[Thromboxane A2 receptor antagonist in asthma therapy]". Nippon Rinsho (in Japanese) 54 (11): 3045–8. PMID 8950952.

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案内

ramatroban