| Identification | Back Directory | [Name]
BEPOTASTINE | [CAS]
125602-71-3 | [Synonyms]
BEPOTASTINE
Bepotastine >
Bepotastine >90%
betotastine besilate
Bepotastine free base
-4-(4-((4-Chlorophenyl)
(190786-43-7) bepotastine
4-[(S)-(4-chlorophenyl)-2-pyridinylMethoxy]-
4-(4-[(1S)(4-CHLOROPHENYL)-2-PYRIDYLMETHOXY]PIPERIDYL)BUTANOIC ACID
4-[4-[(4-Chlorophenyl)pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-
(+)-(S)-4-[4-[1-(4-chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C21H25ClN2O3 | [MDL Number]
MFCD06798155 | [MOL File]
125602-71-3.mol | [Molecular Weight]
388.89 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
4.44±0.10(Predicted) | [color ]
White to Pale Beige |
| Hazard Information | Back Directory | [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.
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| [IC 50]
H1 Receptor | [storage]
Store at -20°C |
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