ArticleBritish journal of pharmacology2013
Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 27 citations in OpenAlex.
- Efficacy of an oral CRTH2 antagonist (AZD1981) in the treatment of chronic rhinosinusitis with nasal polyps in adults: A randomized controlled clinical trial.Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology · 2022Trial
- Effects of an Oral CRTh2 Antagonist (AZD1981) on Eosinophil Activity and Symptoms in Chronic Spontaneous Urticaria.International archives of allergy and immunology · 2019Trial
- Trial
- Efficacy and safety of the CRTh2 antagonist AZD1981 as add-on therapy to inhaled corticosteroids and long-acting βDrug design, development and therapy · 2018Trial
- Pharmacologic activation of Δ133p53α reduces cellular senescence in progeria patients-derived cells.Aging pathobiology and therapeutics · 2025Article
- DP2 receptor activity sensor suited for antagonist screening and measurement of receptor dynamics in real-time.Scientific reports · 2024Article
- Prostaglandin D2 receptor 2 downstream signaling and modulation of type 2 innate lymphoid cells from patients with asthma.PloS one · 2024Article
- Indole-Based and Cyclopentenylindole-Based Analogues Containing Fluorine Group as PotentialPharmaceuticals (Basel, Switzerland) · 2023Review
- In-solution direct oxidative coupling for the integration of sulfur/selenium into DNA-encoded chemical libraries.Chemical science · 2022Article
- Inhibition of the prostaglandin DDiabetologia · 2020Article
- G Protein-Coupled Receptors in Asthma Therapy: Pharmacology and Drug Action.Pharmacological reviews · 2020Review
- Inhibition of CRTH2-mediated Th2 activation attenuates pulmonary hypertension in mice.The Journal of experimental medicine · 2018Article
- Comparison of Effect of Leukotriene Biosynthesis Blockers and Inhibitors of Phosphodiesterase Enzyme in Patients with Bronchial Hyperreactivity.Open access Macedonian journal of medical sciences · 2018Article
- The therapeutic potential of CRTH2/DP2 beyond allergy and asthma.Prostaglandins & other lipid mediators · 2017Review
- CRTH2 antagonists in asthma: current perspectives.Clinical pharmacology : advances and applications · 2017Review
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe discovery of DP2 as a second receptor for PGD2 has prompted the search for antagonists as potential novel therapies based on the associations between PGD2 and disease. Here we describe the biochemical and pharmacological properties of 4-(acetylamino)-3-[(4-chlorophenyl)thio]-2-methyl-1H-indole-1-acetic acid (AZD1981), a novel DP2 receptor antagonist. EXPERIMENTAL APPROACH: Binding to DP2 , functional receptor pharmacology and selectivity were studied in both human and animal systems. KEY
resultsAZD1981 displaced radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4). Binding was reversible, non-competitive and highly selective against a panel of more than 340 other enzymes and receptors, including DP1 (>1000-fold selective). AZD1981 inhibited DP2 -mediated shape change and CD11b up-regulation in human eosinophils, shape change in basophils and chemotaxis of human eosinophils and Th2 cells with similar potency. AZD1981 exhibited good cross-species binding activity against mouse, rat, guinea pig, rabbit and dog DP2 . Evaluation in mouse, rat or rabbit cell systems was not possible as they did not respond to DP2 agonists. Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2 -mediated eosinophil shape change. Such responses were more robust in the guinea pig, where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow. CONCLUSIONS AND IMPLICATIONS: AZD1981 is a DP2 antagonist that blocks functional responses in eosinophils, Th2 cells and basophils. It exhibited similar potency irrespective of the cell type, DP2 agonist or species used. This selective orally active agent is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.
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Registered trials
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