生物活性 | |||
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描述 | Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM. Significant suppression of antigen-induced nasal resistance, nasal secretion, and cell infiltration in nasal mucosa was observed with asapiprant treatment. In addition, treatment with asapiprant suppressed antigen-induced asthmatic responses, airway hyper-responsiveness, and cell infiltration and mucin production in lung. Oral administration of Asapiprant to sheep at 1 and 3 mg/kg significantly suppresses the increase in nasal resistance by 82% and 92%, respectively. Asapiprant at 5 mg/kg suppresses Prostaglandin PGD2-induced nasal resistance by 86%. When orally administered 1 h before the antigen challenge in pigs, Asapiprant (3, 10, and 30 mg/kg) suppresses immediate airway response (IAR) by 52%, 57%, and 96%, and late airway response (LAR) by 67%, 50%, and 79%, respectively. Treatment with Asapiprant in rats at 10 mg/kg significantly reduces airway hyper-responsiveness (AHR), infiltration of inflammatory cells, and mucin production in bronchoalveolar lavage fluid (BALF), although treatment with Asapiprant at 0.1 mg/kg does not have a significant effect on any responses[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.97mL 1.99mL 1.00mL |
19.94mL 3.99mL 1.99mL |
参考文献 |
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