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CGS 21680 is a specific adenosine (A2A) subtype receptor agonist with an IC50 of 5.6 μM for reducing input resistance of the membrane potential. The Ki of CGS 21680 adenosine (A2A) subtype receptor is 27 nM. CGS 21680 has less affinity for A1 and A3 adenosine receptors than A2A- and A2B subtype. CGS 21680 starting at the onset of arthritis (Day 25) improved the clinical signs at Days 26-35 and ameliorated histological states in the joint and paw. The degree of oxidative and nitrosative damage was markedly decreased in CGS 21680-treated mice as exhibited by increased contents of malondialdehyde, formation of nitrotyrosine, and activation of poly (ADP-ribose) polymerase. Plasma levels of proinflammatory cytokines including tumor necrosis factor, interleukin 1ß (IL-1ß) and IL-6 were also decreased by CGS 21680. CGS 21680 also reduced the expression of inducible nitric oxide synthase and cyclooxygenase-2.
Redox Rep. 2022 Dec;27(1):270-278.
Caffeine reduces oxidative stress to protect against hyperoxia-induced lung injury via the adenosine A2A receptor/cAMP/PKA/Src/ERK1/2/p38MAPK pathway
CGS 21680 purchased from AbMole
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Source | PLoS One (2018). Figure 5. CGS 21680 |
| Method | Immunizations | |
| Cell Lines | WT mice | |
| Concentrations | 1 mg/kg | |
| Incubation Time | four weeks | |
| Results | We thus investigated whether administration of an A2a adenosine receptor agonist (CGS 21680) could enhance antibody responses following Pneumovax 23 vaccination in young mice. As shown in Fig 5A and 5B, treatment with the A2a agonist significantly increased mean IgG3 levels at day 7 and 14 post-vaccination |
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | rat |
| Formulation | water |
| Dosages | 10 mg/kg |
| Administration | p.o. |
| Molecular Weight | 499.52 |
| Formula | C23H29N7O6 |
| CAS Number | 120225-54-9 |
| Solubility (25°C) | DMSO 77 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Adenosine Receptor Products |
|---|
| SYN115
Tozadenant (SYN115) is a novel, selective adenosine A(2A) receptor antagonist. |
| CGS 21680 hydrochloride
CGS 21680 hydrochloride is an A2A adenosine receptor agonist with an Ki of 27 nM. |
| Istradefylline
Istradefylline (KW-6002) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. |
| Norisoboldine
Norisoboldine is an isoquinoline alkaloid which acts as an AhR agonist. |
| Theobromine
Theobromine is a methylxanthine found in cocoa beans that inhibits adenosine receptor A1 (AR1) signaling. |
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