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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
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ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
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|CGS 21680 hydrochloride
CGS 21680 hydrochloride is an A2A adenosine receptor agonist with an Ki of 27 nM.
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