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编 号:F042999
分子式:C28H33N5O3
分子量:487.59
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1mg
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生物活性:
Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.

体内研究:
Wy 49051 shows potent activity against histamine-induced lethality in the guinea pig, with ED50 of 1.91 mg/kg by po, 0.70 mg/kg by ip, and 0.01 mg/kg by iv. The duration of action of 24 is also favorable since there is no decrease in oral efficacy up to 18 h posttreatment.

体外研究:
Wy 49051 shows great inhibitory effect on H1, producing 92% inhibition of the histamine-induced contraction of the guinea pig ileum at a concentration 100 nM. Wy 49051 is the most potent compound with 700 times the potency of astemazole, 470 times the potency of chlorpheniramine. Wy 49051 also has high affinity for α1 receptor with IC50 of 8 nM.
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