The adenosine A3 receptor, also known as ADORA3, is an
adenosine receptor, but also denotes the human
gene encoding it.
Function
Adenosine A3 receptors are
G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during
cardiac ischemia, it is involved in the inhibition of
neutrophildegranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death[citation needed].
Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18).
Gene
Multiple transcript variants encoding different isoforms have been found for this gene.[5]
^Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, et al. (June 2007). "Pharmacological characterisation and inhibitory effects of (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol, a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". European Journal of Pharmacology. 564 (1–3): 219–225.
doi:
10.1016/j.ejphar.2007.01.094.
PMID17382926.
^Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S (January 2008). "Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding". ChemMedChem. 3 (1): 111–119.
doi:
10.1002/cmdc.200700173.
hdl:
10261/82277.
PMID18000937.
S2CID7128294.
^Courtney L. Fisher, Matteo Pavan, Veronica Salmaso, Robert F. Keyes, Tina C. Wan, Balaram Pradhan, Zhan-Guo Gao, Brian C. Smith, Kenneth A. Jacobson and John A. Auchampach. [<
https://doi.org/10.1124/molpharm.123.000784> "Extrahelical binding site for a 1H-imidazo[4,5-c]quinolin-4-amine A3 adenosine receptor positive allosteric modulator on helix 8 and distal portions of transmembrane domains 1 and 7"]
^Mikus EG, Szeredi J, Boer K, Tímári G, Finet M, Aranyi P, Galzin AM (January 2013). "Evaluation of SSR161421, a novel orally active adenosine A3 receptor antagonist on pharmacology models". European Journal of Pharmacology. 699 (1–3): 172–179.
doi:
10.1016/j.ejphar.2012.11.049.
PMID23219796.
^Mikus EG, Boér K, Timári G, Urbán-Szabó K, Kapui Z, Szeredi J, et al. (January 2013). "Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". European Journal of Pharmacology. 699 (1–3): 62–66.
doi:
10.1016/j.ejphar.2012.11.046.
PMID23219789.
Broussas M, Cornillet-Lefèbvre P, Potron G, Nguyên P (July 2002). "Adenosine inhibits tissue factor expression by LPS-stimulated human monocytes: involvement of the A3 adenosine receptor". Thrombosis and Haemostasis. 88 (1): 123–130.
doi:
10.1055/s-0037-1613164.
PMID12152652.
S2CID3118696.
"Adenosine Receptors: A3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from
the original on 2020-11-30. Retrieved 2008-11-25.
The adenosine A3 receptor, also known as ADORA3, is an
adenosine receptor, but also denotes the human
gene encoding it.
Function
Adenosine A3 receptors are
G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during
cardiac ischemia, it is involved in the inhibition of
neutrophildegranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death[citation needed].
Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18).
Gene
Multiple transcript variants encoding different isoforms have been found for this gene.[5]
^Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, et al. (June 2007). "Pharmacological characterisation and inhibitory effects of (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol, a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". European Journal of Pharmacology. 564 (1–3): 219–225.
doi:
10.1016/j.ejphar.2007.01.094.
PMID17382926.
^Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S (January 2008). "Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding". ChemMedChem. 3 (1): 111–119.
doi:
10.1002/cmdc.200700173.
hdl:
10261/82277.
PMID18000937.
S2CID7128294.
^Courtney L. Fisher, Matteo Pavan, Veronica Salmaso, Robert F. Keyes, Tina C. Wan, Balaram Pradhan, Zhan-Guo Gao, Brian C. Smith, Kenneth A. Jacobson and John A. Auchampach. [<
https://doi.org/10.1124/molpharm.123.000784> "Extrahelical binding site for a 1H-imidazo[4,5-c]quinolin-4-amine A3 adenosine receptor positive allosteric modulator on helix 8 and distal portions of transmembrane domains 1 and 7"]
^Mikus EG, Szeredi J, Boer K, Tímári G, Finet M, Aranyi P, Galzin AM (January 2013). "Evaluation of SSR161421, a novel orally active adenosine A3 receptor antagonist on pharmacology models". European Journal of Pharmacology. 699 (1–3): 172–179.
doi:
10.1016/j.ejphar.2012.11.049.
PMID23219796.
^Mikus EG, Boér K, Timári G, Urbán-Szabó K, Kapui Z, Szeredi J, et al. (January 2013). "Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". European Journal of Pharmacology. 699 (1–3): 62–66.
doi:
10.1016/j.ejphar.2012.11.046.
PMID23219789.
Broussas M, Cornillet-Lefèbvre P, Potron G, Nguyên P (July 2002). "Adenosine inhibits tissue factor expression by LPS-stimulated human monocytes: involvement of the A3 adenosine receptor". Thrombosis and Haemostasis. 88 (1): 123–130.
doi:
10.1055/s-0037-1613164.
PMID12152652.
S2CID3118696.
"Adenosine Receptors: A3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from
the original on 2020-11-30. Retrieved 2008-11-25.