BEPOTASTINE
BEPOTASTINE Basic information
- Product Name:
- BEPOTASTINE
- Synonyms:
-
- 4-(4-[(1S)(4-CHLOROPHENYL)-2-PYRIDYLMETHOXY]PIPERIDYL)BUTANOIC ACID
- 1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-
- betotastine besilate
- 4-[4-[(4-Chlorophenyl)pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
- (+)-(S)-4-[4-[1-(4-chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid
- 4-[(S)-(4-chlorophenyl)-2-pyridinylMethoxy]-
- -4-(4-((4-Chlorophenyl)
- BEPOTASTINE
- CAS:
- 125602-71-3
- MF:
- C21H25ClN2O3
- MW:
- 388.89
- EINECS:
- 200-258-5
- Mol File:
- 125602-71-3.mol
BEPOTASTINE 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
BEPOTASTINE 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
BEPOTASTINESupplier
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- +86 (0) 571 85 58 67 18
- Tel
- 001-857-928-2050 or 1-888-588-9418
- sales@chemreagents.com
- Tel
- 1-(800)-881-8210
- inquiries@lgmpharma.com
- Tel
- 025-83697070
- info@chemlin.com.cn