生物活性 | |||
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描述 | D prostanoid receptor 2 (DP2) is selectively expressed by T helper 2 (Th2) lymphocytes, eosinophils, and basophils and mediates recruitment and activation of these cell types in response to prostaglandin D2 (PGD2)[1]. OC000459 is a potent, selective, and orally active DP2 antagonist. It potently displaces [3H] PGD2 from human recombinant DP2 (Ki = 13 nM), rat recombinant DP2 (Ki = 3 nM), and human native DP2 (Ki = 4 nM). OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells[1]. OC000459 was found to be orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13, 14-dihydro-15-keto-PGD2 (DK-PGD2) in this species (ED50 = 0.04 mg/kg p.o.) and airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50 = 0.01 mg/kg p.o.)[1]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00290381 | Allergic Rhinitis | Phase 1 | Completed | - | United Kingdom ... 展开 >> National Heart & Lung Institute Clinical Studies Unit London, United Kingdom, SW3 6HP 收起 << |
NCT02660489 | Asthma Rhinov... 展开 >>irus Picornaviridae Infections Common Cold 收起 << | Phase 2 | Unknown | February 2018 | United Kingdom ... 展开 >> St Mary's Hospital Recruiting London, Greater London, United Kingdom, W2 1PG Contact: Hugo Farne, BMBCh MA 07590 250487 asthma.trial@imperial.ac.uk Contact: Maria-Belén Trujillo-Torralbo, BSc 07590 250487 asthma.trial@imperial.ac.uk 收起 << |
NCT00697281 | Allergic Rhinitis | Phase 2 | Completed | - | Austria ... 展开 >> Allergie Zentrum Wien West, Vienna Challenge Chamber Vienna, Austria, 1150 VIENNA 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.87mL 0.57mL 0.29mL |
14.35mL 2.87mL 1.44mL |
28.71mL 5.74mL 2.87mL |
参考文献 |
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