Short description: 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. 200. pp. 151–99. doi:10.1007/978-3-642-13443-2_6. ISBN 978-3-642-13442-5.
- ↑ 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. 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.
- ↑ Jiang, Jie; Seel, Catharina Julia; Temirak, Ahmed; Namasivayam, Vigneshwaran; Arridu, Antonella; Schabikowski, Jakub; Baqi, Younis; Hinz, Sonja et al. (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. https://pubmed.ncbi.nlm.nih.gov/30835463/.
- ↑ El Maatougui, Abdelaziz; Azuaje, Jhonny; González-Gómez, Manuel; Miguez, Gabriel; Crespo, Abel; Carbajales, Carlos; Escalante, Luz; García-Mera, Xerardo et al. (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. https://pubmed.ncbi.nlm.nih.gov/26824742/.
- ↑ Prieto-Díaz, Rubén; González-Gómez, Manuel; Fojo-Carballo, Hugo; Azuaje, Jhonny; El Maatougui, Abdelaziz; Majellaro, Maria; Loza, María I.; Brea, José et al. (2022-12-14). "Exploring the Effect of Halogenation in a Series of Potent and Selective A 2B Adenosine Receptor Antagonists" (in en). Journal of Medicinal Chemistry 66 (1): 890–912. doi:10.1021/acs.jmedchem.2c01768. ISSN 0022-2623. PMID 36517209.
- ↑ Borodovsky, Alexandra; Barbon, Christine M.; Wang, Yanjun; Ye, Minwei; Prickett, Laura; Chandra, Dinesh; Shaw, Joseph; Deng, Nanhua et al. (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. PMID 32727810.
Pharmacomodulation |
|---|
| Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Partial agonist
- Antagonist
- Inverse agonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- ♦ Transporter [Reuptake vs Efflux]: Enhancer (RE)
- Inhibitor (RI)
- Releaser (RA)
- ♦ Miscellaneous: Precursor
- Cofactor
|
|---|
| Classes | | Enzyme | see Enzyme inhibition |
|---|
| Ion channel | See Ion channel modulators |
|---|
Receptor & transporter | | BA/M | | Adrenergic |
- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2)
- β)
- Norepinephrine reuptake inhibitor (NRI)
|
|---|
| Dopaminergic |
- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
|
|---|
| Histaminergic |
- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
|
|---|
| Serotonergic |
- Serotonin receptor agonist
- Serotonin receptor antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
|
|---|
|
|---|
| AA | | GABAergic |
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
|
|---|
| Glutamatergic |
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
|
|---|
|
|---|
| Cholinergic |
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
|
|---|
| Cannabinoidergic |
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
- Endocannabinoid enhancer (eCBE)
- Endocannabinoid reuptake inhibitor (eCBRI)
|
|---|
| Opioidergic |
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
- Enkephalinase inhibitor
|
|---|
| Other |
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
|
|---|
|
|---|
| Miscellaneous |
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
|
|---|
|
|---|
 | Original source: https://en.wikipedia.org/wiki/Adenosine receptor antagonist. Read more |