Home Neuronal Signaling Histamine Receptor antagonist - COVID-19 inhibitor Bepotastine Besilate For research use only.

Bepotastine Besilate

Synonyms: TAU 284

Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

Bepotastine Besilate Chemical Structure

Bepotastine Besilate Chemical Structure

CAS No. 190786-44-8

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Bepotastine Besilate Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
Targets
Histamine H1 receptor [1]
5.7(pIC50)
In vitro
In vitro 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. [2] Bepotastine besilate (100 mM) suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured dorsal root ganglion neurons and cultured neutrophils. [3] 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. [4]
In Vivo
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. [2] 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). [3] 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%. [4] 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. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01925313 Completed
Healthy
HK inno.N Corporation
 December 2012 Phase 1
NCT01425632 Completed
Perennial Allergic Rhinitis
Mitsubishi Tanabe Pharma Corporation
 August 2011 Phase 3

Chemical Information & Solubility

Molecular Weight 547.06 Formula

C21H25ClN2O3.C6H6O3S
CAS No. 190786-44-8 SDF Download Bepotastine Besilate SDF
Smiles C1CN(CCC1OC(C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O.C1=CC=C(C=C1)S(=O)(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 109 mg/mL ( (199.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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