Adenosine receptor antagonist
Class of drugs
An adenosine receptor antagonist is a drug which acts as an antagonist of one or more of the adenosine receptors.[1] The best known are xanthines and their derivatives (natural: caffeine,[2] theophylline,[3] and theobromine; and synthetic: PSB-1901[4]), but there are also non-xanthine representatives (e.g. ISAM-140,[5] ISAM-R316,[6] Etrumadenant, and AZD-4635[7])
See also
- Adenosine receptor agonist
- Adenosine reuptake inhibitor
References
- ^ Müller, CE; Jacobson, KA (2011). Xanthines as adenosine receptor antagonists. Handbook of Experimental Pharmacology. Vol. 200. pp. 151–99. doi:10.1007/978-3-642-13443-2_6. ISBN 978-3-642-13442-5. PMC 3882893. PMID 20859796.
- ^ Rivera-Oliver, Marla; Díaz-Ríos, Manuel (April 2014). "Using caffeine and other adenosine receptor antagonists and agonists as therapeutic tools against neurodegenerative diseases: A review". Life Sciences. 101 (1–2): 1–9. doi:10.1016/j.lfs.2014.01.083. PMC 4115368. PMID 24530739.
- ^ Hauber, W.; Muenkle, M. (July 1996). "The adenosine receptor antagonist theophylline induces a monoamine-dependent increase of the anticataleptic effects of NMDA receptor antagonists". Naunyn-Schmiedeberg's Archives of Pharmacology. 354 (2): 179–186. doi:10.1007/BF00178718. PMID 8857595. S2CID 21765941.
- ^ Jiang, Jie; Seel, Catharina Julia; Temirak, Ahmed; Namasivayam, Vigneshwaran; Arridu, Antonella; Schabikowski, Jakub; Baqi, Younis; Hinz, Sonja; Hockemeyer, Jörg; Müller, Christa E. (2019-04-25). "A2B Adenosine Receptor Antagonists with Picomolar Potency". Journal of Medicinal Chemistry. 62 (8): 4032–4055. doi:10.1021/acs.jmedchem.9b00071. ISSN 1520-4804. PMID 30835463. S2CID 73472174.
- ^ El Maatougui, Abdelaziz; Azuaje, Jhonny; González-Gómez, Manuel; Miguez, Gabriel; Crespo, Abel; Carbajales, Carlos; Escalante, Luz; García-Mera, Xerardo; Gutiérrez-de-Terán, Hugo; Sotelo, Eddy (2016-03-10). "Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes". Journal of Medicinal Chemistry. 59 (5): 1967–1983. doi:10.1021/acs.jmedchem.5b01586. ISSN 1520-4804. PMID 26824742.
- ^ Prieto-Díaz, Rubén; González-Gómez, Manuel; Fojo-Carballo, Hugo; Azuaje, Jhonny; El Maatougui, Abdelaziz; Majellaro, Maria; Loza, María I.; Brea, José; Fernández-Dueñas, Víctor; Paleo, M. Rita; Díaz-Holguín, Alejandro; Garcia-Pinel, Beatriz; Mallo-Abreu, Ana; Estévez, Juan C.; Andújar-Arias, Antonio (2022-12-14). "Exploring the Effect of Halogenation in a Series of Potent and Selective A 2B Adenosine Receptor Antagonists". Journal of Medicinal Chemistry. 66 (1): 890–912. doi:10.1021/acs.jmedchem.2c01768. ISSN 0022-2623. PMC 9841532. PMID 36517209. S2CID 254759241.
- ^ Borodovsky, Alexandra; Barbon, Christine M.; Wang, Yanjun; Ye, Minwei; Prickett, Laura; Chandra, Dinesh; Shaw, Joseph; Deng, Nanhua; Sachsenmeier, Kris; Clarke, James D.; Linghu, Bolan; Brown, Giles A.; Brown, James; Congreve, Miles; Cheng, Robert Ky (July 2020). "Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity". Journal for Immunotherapy of Cancer. 8 (2): e000417. doi:10.1136/jitc-2019-000417. ISSN 2051-1426. PMC 7394305. PMID 32727810.
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Pharmacomodulation
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Partial agonist
- Antagonist
- Inverse agonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- ♦ Miscellaneous: Precursor
- Cofactor
| Enzyme | see Enzyme inhibition |
|---|---|
| Ion channel | See Ion channel modulators |
| Receptor & transporter | |
| Miscellaneous |
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