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编 号:F096962
分子式:C21H25ClN2O3
分子量:388.89
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CAS No: 125602-71-3
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生物活性:
Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.
体内研究:
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.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.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.Animal Model:Guinea pigs (6-week-old).
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.
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.
体外研究:
Bepotastine (10, 100, 1000 μM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 μM.Bepotastine (50 μM; 1 h) suppresses the expression of NGF mRNA in NHEKs.