ArticleBiochemical pharmacology2005
CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors.
Article in Biochemical pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
38 citing papers in PubMed, 82 citations in OpenAlex.
- Decoding the lncRNA landscape in bovine mastitis: insights into immune regulation and gene networks underlying host response.Journal of animal science and biotechnology · 2026Article
- Cysteinyl Leukotrienes in Allergic Inflammation.Annual review of pathology · 2025Review
- Time to Rethink Bronchiolitis Obliterans Syndrome Following Lung or Hematopoietic Cell Transplantation in Pediatric Patients.Cancers · 2024Review
- Efficacy and Safety of Montelukast+Levocetirizine Combination Therapy Compared to Montelukast Monotherapy for Allergic Rhinitis in Children.Allergy, asthma & immunology research · 2024Article
- Macrophage P2Y6 Receptor Signaling Selectively Activates NFATC2 and Suppresses Allergic Lung Inflammation.Journal of immunology (Baltimore, Md. : 1950) · 2022Article
- Leukotriene receptor antagonists and risk of neuropsychiatric events in children, adolescents and young adults: a self-controlled case series.The European respiratory journal · 2022Article
- Article
- Montelukast Inhibits Platelet Activation Induced by Plasma From COVID-19 Patients.Frontiers in pharmacology · 2022Article
- 1,4-dihydroxy quininib modulates the secretome of uveal melanoma tumour explants and a marker of oxidative phosphorylation in a metastatic xenograft model.Frontiers in medicine · 2022Article
- Classification models and SAR analysis on CysLT1 receptor antagonists using machine learning algorithms.Molecular diversity · 2021Article
- Zafirlukast is a broad-spectrum thiol isomerase inhibitor that inhibits thrombosis without altering bleeding times.British journal of pharmacology · 2021Article
- P2Y6 signaling in alveolar macrophages prevents leukotriene-dependent type 2 allergic lung inflammation.The Journal of clinical investigation · 2019Article
- Cysteinyl Leukotrienes as Potential Pharmacological Targets for Cerebral Diseases.Mediators of inflammation · 2017Review
- Purinergic Signaling in Mast Cell Degranulation and Asthma.Frontiers in pharmacology · 2017Review
- Prostaglandin D2 and leukotriene E4 synergize to stimulate diverse TH2 functions and TH2 cell/neutrophil crosstalk.The Journal of allergy and clinical immunology · 2015Article
- Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7.British journal of pharmacology · 2014Review
- Role of cysteinyl leukotriene signaling in a mouse model of noise-induced cochlear injury.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- Is GPR17 a P2Y/leukotriene receptor? examination of uracil nucleotides, nucleotide sugars, and cysteinyl leukotrienes as agonists of GPR17.The Journal of pharmacology and experimental therapeutics · 2013Article
- Cysteinyl leukotriene receptors, old and new; implications for asthma.Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology · 2012Review
- Leukotriene E4 activates human Th2 cells for exaggerated proinflammatory cytokine production in response to prostaglandin D2.Journal of immunology (Baltimore, Md. : 1950) · 2012Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
Montelukast and pranlukast are orally active leukotriene receptor antagonists selective for the CysLT1 receptor. Conversely, the hP2Y(1,2,4,6,11,12,13,14) receptors represent a large family of GPCRs responding to either adenine or uracil nucleotides, or to sugar-nucleotides. Montelukast and pranlukast were found to inhibit nucleotide-induced calcium mobilization in a human monocyte-macrophage like cell line, DMSO-differentiated U937 (dU937). Montelukast and pranlukast inhibited the effects of UTP with IC50 values of 7.7 and 4.3 microM, respectively, and inhibited the effects of UDP with IC50 values of 4.5 and 1.6 microM, respectively, in an insurmountable manner. Furthermore, ligand binding studies using [3H]LTD4 excluded the possibility of orthosteric nucleotide binding to the CysLT1 receptor. dU937 cells were shown to express P2Y2, P2Y4, P2Y6, P2Y11, P2Y13 and P2Y14 receptors. Therefore, these antagonists were studied functionally in a heterologous expression system for the human P2Y receptors. In 1321N1 astrocytoma cells stably expressing human P2Y(1,2,4,6) receptors, CysLT1 antagonists inhibited both the P2Y agonist-induced activation of phospholipase C and intracellular Ca2+ mobilization. IC50 values at P2Y1 and P2Y6 receptors were <1 microM. In control astrocytoma cells expressing an endogenous M3 muscarinic receptor, 10 microM montelukast had no effect on the carbachol-induced rise in intracellular Ca2+. These data demonstrated that CysLT1 receptor antagonists interact functionally with signaling pathways of P2Y receptors, and this should foster the study of possible implications for the clinical use of these compounds in asthma or in other inflammatory conditions.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.