物质信息
ID:4531
名称和标识
IUPAC传统名
@bepotastine
别名
bepotastineBepotastineBetotastine besilateTAU-284DSBepotastine besilate
商标名
Talion
IUPAC标准名
4-{4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}butanoic acid
化合物性质
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描述信息
Drug Groups
approved; investigational
Description
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and uriticaria/puritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion®. It is currently undergoing trials in the U.S.
Indication
For the treatment of allergic conjunctivitis and uriticaria/puritus.
Pharmacology
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. It has a stabilizing effect on mast cells, and it suppresses the migration of eosinophils into inflamed tissues. Bepotastine is under investigation in an eye drop formulation by Ista for the treatment of allergic conjunctivitis. An oral formulation of this drug is approved in Japan for the treatment of allergic conjunctivitis and uriticaria/puritus. Ista Pharm. filed an IND with the FDA for bepotastine in December of 2006.
Affected Organisms
Humans and other mammals
Absorption
High oral absorption
References
•
Ohashi R, Kamikozawa Y, Sugiura M, Fukuda H, Yabuuchi H, Tamai I: Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate. Drug Metab Dispos. 2006 May;34(5):793-9. Epub 2006 Feb 2.
[Pubmed]
•
Andoh T, Kuraishi Y: Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice. Eur J Pharmacol. 2006 Oct 10;547(1-3):59-64. Epub 2006 Jul 25.
[Pubmed]
External Links
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参考文献
• Andoh T, Kuraishi Y: Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice. Eur J Pharmacol. 2006 Oct 10;547(1-3):59-64. Epub 2006 Jul 25. Pubmed
• Ohashi R, Kamikozawa Y, Sugiura M, Fukuda H, Yabuuchi H, Tamai I: Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate. Drug Metab Dispos. 2006 May;34(5):793-9. Epub 2006 Feb 2. Pubmed