The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.
Antagonists of the Platelet P2T Receptor: A Novel Approach to Antithrombotic Therapy
Abstract
The platelet P2T receptor plays a major role in platelet aggregation, and its antagonists are predicted to have significant therapeutic potential as antithrombotic agents. We have explored analogues of adenosine triphosphate (ATP), which is a weak, nonselective but competitive P2T receptor antagonist. Modification of the polyphosphate side chain to prevent breakdown to the agonist adenosine diphosphate (ADP) and substitution of the adenine moiety to enhance affinity and selectivity for the P2T receptor led to the identification of 10e (AR-C67085MX), having an IC50 of 2.5 nM against ADP-induced aggregation of human platelets. Compound 10e was the first very potent antagonist of the P2T receptor, with a selectivity for that subtype of the P2 receptor family of >1000-fold. Further modification of the structure produced compound 10l (AR-C69931MX) having an IC50 of 0.4 nM. In vivo, at maximally effective antithrombotic doses, there is little prolongation of bleeding time (1.4-fold), which is in marked contrast to the 5-6-fold found with GPIIb/IIIa antagonists.
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Citations
Cites
Extracellular ATP: effects, sources and fate
Gordon, J. L. (1986) · Biochemical Journal · doi:10.1042/bj2330309 · Cited by 1,658
Is there a basis for distinguishing two types of P2-purinoceptor?
Burnstock, G., & Kennedy, C. (1985) · General Pharmacology: The Vascular System · doi:10.1016/0306-3623(85)90001-1 · Cited by 1,365
Non-genomic and genomic effects of steroids on neural activity
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Molecular Basis for ADP-induced Platelet Activation
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Self-citationPurinergic approaches in experimental therapeutics
(1997) · European Journal of Medicinal Chemistry · doi:10.1016/s0223-5234(97)82766-3 · Cited by 255
P2 Purinoceptors: Historical Perspective and Classification
Burnstock, G. (2007) · Novartis Foundation symposium · doi:10.1002/9780470514900.ch1 · Cited by 142
FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T‐purinoceptors
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Wang, J., Sánchez-Roselló, M., Aceña, J. L., del Pozo, C., Sorochinsky, A. E., Fustero, S., Soloshonok, V. A., & Liu, H. (2014) · Chemical Reviews · doi:10.1021/cr4002879 · Cited by 4,847
Abbracchio, M. P., Burnstock, G., Boeynaems, J.-M., Barnard, E. A., Boyer, J. L., Kennedy, C., Knight, G. E., Fumagalli, M., Gachet, C., Jacobson, K. A., et al. (2006) · Pharmacological Reviews · doi:10.1124/pr.58.3.3 · Cited by 1,281
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Extracellular ATP or ADP Induce Chemotaxis of Cultured Microglia through Gi/o-Coupled P2Y Receptors
Honda, S., Sasaki, Y., Ohsawa, K., Imai, Y., Nakamura, Y., Inoue, K., & Kohsaka, S. (2001) · The Journal of Neuroscience · doi:10.1523/jneurosci.21-06-01975.2001 · Cited by 561
Ciana, P., Fumagalli, M., Trincavelli, M. L., Verderio, C., Rosa, P., Lecca, D., Ferrario, S., Parravicini, C., Capra, V., Gelosa, P., et al. (2006) · The EMBO Journal · doi:10.1038/sj.emboj.7601341 · Cited by 438
Metadata
- Authors
- Ingall, A. H., Dixon, J., Bailey, A., Coombs, M. E., Cox, D., McInally, J. I., Hunt, S. F., Kindon, N. D., Teobald, B. J., Willis, P. A., Humphries, R. G., Leff, P., Clegg, J. A., Smith, J. A., & Tomlinson, W.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1999-01-01
- Volume
- 42
- Issue
- 2
- Pages
- 213-220
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1986775812
- Cited by
- 283
- References
- 7
- FWCI
- 10.74
- Type
- journal article
- Language
- en
- Open access
- closed
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