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Competitive and selective antagonism of P2Y1 receptors by N6‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate
Open accessAbstract
The antagonist activity of N6‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate (N6MABP) has been examined at the phospholipase C‐coupled P2Y 1 receptor of turkey erythrocyte membranes. N6MABP antagonized 2MeSATP‐stimulated inositol phosphate hydrolysis with a potency approximately 20 fold greater than the previously studied parent molecule, adenosine 3′,5′‐bisphosphate. The P2Y 1 receptor antagonism observed with N6MABP was competitive as revealed by Schild analysis (pK B=6.99±0.13). Whereas N6MABP was an antagonist at the human P2Y 1 receptor, no antagonist effect of N6MABP was observed at the human P2Y 2, human P2Y 4 or rat P2Y 6 receptors.
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Cited by
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Takasaki, J., Saito, T., Taniguchi, M., Kawasaki, T., Moritani, Y., Hayashi, K., & Kobori, M. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m408846200 · Cited by 396
Delekate, A., Füchtemeier, M., Schumacher, T., Ulbrich, C., Foddis, M., & Petzold, G. C. (2014) · Nature Communications · doi:10.1038/ncomms6422 · Cited by 332
P2Y1 receptor blockade normalizes network dysfunction and cognition in an Alzheimer’s disease model
Reichenbach, N., Delekate, A., Breithausen, B., Keppler, K., Poll, S., Schulte, T., Peter, J., Plescher, M., Hansen, J. N., Blank, N., et al. (2018) · Journal of Experimental Medicine · doi:10.1084/jem.20171487 · Cited by 131
Kittner, H., Franke, H., Fischer, W., Schultheis, N., Krügel, U., & Illes, P. (2003) · Neuropsychopharmacology · doi:10.1038/sj.npp.1300043 · Cited by 71
Metadata
- Authors
- Boyer, J. L., Mohanram, A., Camaioni, E., Jacobson, K. A., & Harden, T. K.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 1998-05
- Volume
- 124
- Issue
- 1
- Pages
- 1-3
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2036146605
- Cited by
- 199
- References
- 0
- FWCI
- 5.03
- Type
- journal article
- Language
- en
- Open access
- bronze
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- CoChat. (2026). Citation check: Competitive and selective antagonism of P2Y1 receptors by N6‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate. https://app.cochat.ai/papers/10.1038/sj.bjp.0701837
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- Boyer, J. L., Mohanram, A., Camaioni, E., Jacobson, K. A., & Harden, T. K. (1998). Competitive and selective antagonism of P2Y1 receptors by N6‐methyl 2′‐deoxyadenosine 3′,5′‐bisphosphate. British Journal of Pharmacology. https://doi.org/10.1038/sj.bjp.0701837
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
