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BEPOTASTINE

Product NameBEPOTASTINE
CAS125602-71-3
MFC21H25ClN2O3
MW388.89
EINECS200-258-5
MOL File125602-71-3.mol

Chemical Properties

Melting point	56 - 58°C
Boiling point	546.8±50.0 °C(Predicted)
Density	1.26
storage temp.	-20°C Freezer, Under inert atmosphere
solubility	DMSO (Slightly), Methanol (Slightly)
pka	4.44±0.10(Predicted)
form	Solid
color	White to Pale Beige
InChIKey	YWGDOWXRIALTES-NRFANRHFSA-N
SMILES	[C@@H](C1N=CC=CC=1)(C1C=CC(=CC=1)Cl)OC1CCN(CC1)CCCC(=O)O

Usage And Synthesis

Uses

Bepotastine is a histamine H1 receptor antagonist. Bepotastine suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).

Definition

ChEBI: An ether that is (S)-(4-chlorophenyl)(pyridin-2-yl)methanol in which the hydroxyl hydrogen is substituted by a 1-(3-carboxypropyl)piperidin-4-yl group. A topical, selective and non-sedating histamine (H1) receptor anta onist used (as its benzenesulfonate salt) for treatment of itching associated with allergic conjunctivitis.

in vivo

Bepotastine (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration^[1].
Bepotastine (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control^[3].
Bepotastine (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash^[3].

Animal Model:	Guinea pigs (6-week-old)^[1].
Dosage:	10 g/L (1.0% (w/v)) for 10 μL.
Administration:	Eye drop; 3 times at intervals of 20 min (in one eye).
Result:	Inhibited PAF-induced conjunctival eosinophil infiltration.

Animal Model:	Male BALB/c mice(12-week-old); NC/Nga mice^[3].
Dosage:	3, 10 mg/kg
Administration:	Oral administration; once (1 h before induces scratching behavior of Male BALB/c mice).
Result:	Significantly inhibited histamine-mediated scratching behavior in male BALB/c mice. Significantly suppressed serum LTB 4 levels in NC/Nga mice with a rash.

IC 50

H₁ Receptor

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