AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1.
1.Schmidt JA, Bell FM, Akam E, Marshall C, Dainty IA, Heinemann A, Dougall IG, Bonnert RV, Sargent CA. (2013) Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma.. Br J Pharmacol, 168 (7):(1626-38). [PMID:23146091]
2.Kuna P, Bjermer L, Tornling G. (2016) Two Phase II randomized trials on the CRTh2 antagonist AZD1981 in adults with asthma.. Drug Des Devel Ther, 10 (3):(2759-70). [PMID:27621597]
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4.Oliver ET, Chichester K, Devine K, Sterba PM, Wegner C, Vonakis BM, Saini SS. (2019) Effects of an Oral CRTh2 Antagonist (AZD1981) on Eosinophil Activity and Symptoms in Chronic Spontaneous Urticaria.. Int Arch Allergy Immunol, 179 (1):(21-30). [PMID:30879003]
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A2213091