Catalog No.S3037 Synonyms: TAU 284
Molecular Weight(MW): 547.06
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
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|Description||Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.|
The flux ratios of [14C]Bepotastine (5 μM) in LLC-GA5-COL150 cells are significantly greater than those in LLC-PK1, showing that the B-to-A flux exceeds those in the other direction in LLC-GA5-COL150 cells. Bepotastine stimulates P-gp-mediated ATP hydrolysis with Km, Vmax, and Vmax/Km values of 1.25 mM, 108 nmol/min/mg protein, and 0.087 mL/min/mg protein, respectively.  Bepotastine besilate (100 mM) suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured dorsal root ganglion neurons and cultured neutrophils.  Bepotastine (100 μM) dose-dependently inhibits chemotaxis of cultured guinea pig peritoneal eosinophils induced by LTB4. Bepotastine (1 mM) significantly reduces A23187-induced histamine release of cultured rat peritoneal mast cells. 
|In vivo||Bepotastine (0.8 mg/kg) administrated in WT and P-gp KO mice results in the plasma total concentrations 580 ng/mL and 467 ng/mL at 6 min after dosing, respectively, and the plasma protein binding with 41.1% and 45.9%. The absorption of [14C]Bepotastine from the proximal region in the presence and absence of verapamil is 63.0% and 72.4%, respectively, and that from the distal region is 10.9% and 62.7%, respectively.  Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site). Bepotastine besilate (1 mg/kg-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B(4) (0.03 nmol/site).  Bepotastine besilate significantly inhibits conjunctival vascular hyperpermeability in a dose-dependent manner in guinea pig allergic conjunctivitis models with maximal effect for Bepotastine besilate 1.5%.  Bepotastine (3 mg/kg and 10 mg/kg) effectively inhibits the compound 48/80-induced scratching behavior of BALB/c mice 1 hour after oral administration. Bepotastine (10 mg/kg) also significantly inhibits the scratching behavior and suppresses the serum LTB(4) levels in atopic dermatitis model NC/Nga mice. |
-  Da Prada M, et al. J Pharmacol Exp Ther, 1989, 248(1), 400-414.
-  Ohashi R, et al. Drug Metab Dispos, 2006, 34(5), 793-799.
-  Andoh T, et al. Eur J Pharmacol, 2006, 547(1-3), 59-64.
|In vitro||DMSO||109 mg/mL (199.24 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01900054||Completed||Perennial Allergic Rhinitis||Mitsubishi Tanabe Pharma Corporation||June 2013||Phase 3|
|NCT01861522||Completed||Perennial Allergic Rhinitis||Mitsubishi Tanabe Pharma Corporation||April 2013||Phase 3|
|NCT01840605||Completed||Dermatitis|Atopic||Mitsubishi Tanabe Pharma Corporation||March 2013||Phase 3|
|NCT01753739||Completed||Seasonal Allergic Rhinitis||Bausch & Lomb Incorporated||January 2013||Phase 2|
|NCT01578278||Completed||Seasonal Allergic Rhinitis||Bausch & Lomb Incorporated||December 2011||Phase 2|
|NCT01443442||Completed||Allergic Conjunctivitis||Southern California College of Optometry||October 2011||Phase 4|
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