In vitro
AM1241 is a CB(2) receptor-selective agonist. AM1241 displays high affinity at the human CB2 receptor with a Ki value of about 7nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker. In FLIPR assays, AM1241 exhibits antagonist activity, blocking the agonist CP 55,940-evoked Ca2+ response in a concentration dependent manner with a Kb value of 63nM. The antinociceptive actions of AM1241 are blocked by the CB(2) receptor-selective antagonist AM630, but not by the CB(1) receptor-selective antagonist AM251. AM1241 also produces antinociception when injected systemically (intraperitoneally). AM1241 dose-dependently blocks the agonist activity of CP55,940 (4nM) and the inverse agonist activity of SR144528 (100nM) at the human CB2 receptor with Kb values at 27 and 11nM, respectively.
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