ZM241385 is a novel non-xanthine adenosine receptor antagonist with selectivity for the A2a receptor subtype. ZM-241385 significantly blunts the hypotensive effects of CCPA and NECA without altering the bradycardia induced by these agonists. It blocks the infarct size-reducing effects(cardioprotective effects) of this two distinct adenosine receptor agonists.
In vitro: ZM-241385 exhibits high potency for A2a receptor-mediated effects versus A1 receptor-mediated effects. A2AR agonist CGS21680 dramatically up-regulated A2AR mRNA; this response was reversed by concurrent exposure to ZM241385.
|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.
|Solubility||DMSO 65 mg/mL|
The A2a/A2b receptor antagonist ZM-241385 blocks the cardioprotective effect of adenosine agonist pretreatment in in vivo rat myocardium.
Lasley RD, et al. Am J Physiol Heart Circ Physiol. 2007 Jan;292(1):H426-31. PMID: 16980350.
|Related Adenosine Receptor Products|
CPI-444 is a potent and selective inhibitor of A2A receptor (A2AR) induces antitumor responses.
Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing.
CGS 21680 is a selective adenosine receptor agonist for A2A and A3 with Ki of 15 ng/mL and 37 ng/mL, respectively.
Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM.
|CGS 21680 hydrochloride
CGS 21680 hydrochloride is an A2A adenosine receptor agonist with an Ki of 27 nM.
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