AM-1241 is a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 3.4nM at CB2 and 80x selectivity over the related CB1 receptor. AM1241 exhibits high affinity and selectivity for CB2 receptors. It also exhibits high potency in vivo. AM1241 dose-dependently reversed tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. AM1241 also inhibited flinching and thermal hyperalgesia produced by hind paw capsaicin injection. AM1241 was also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that AM1241 reverses sensory hypersensitivity independent of actions at CB1 receptors. Treatment with AM-1241 reduced both spontaneous and evoked pain, as well as reducing the bone loss and subsequent fractures due to the tumor.
|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 100 mg/mL|
Species-specific in vitro pharmacological effects of the cannabinoid receptor 2 (CB2) selective ligand AM1241 and its resolved enantiomers.
Bingham B, et al. Br J Pharmacol. 2007 Aug;151(7):1061-70. PMID: 17549048.
The CB2 cannabinoid agonist AM-1241 prolongs survival in a transgenic mouse model of amyotrophic lateral sclerosis when initiated at symptom onset.
Shoemaker JL, et al. J Neurochem. 2007 Apr;101(1):87-98. PMID: 17241118.
In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor?
Yao BB, et al. Br J Pharmacol. 2006 Sep;149(2):145-54. PMID: 16894349.
Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS.
Ibrahim MM, et al. Proc Natl Acad Sci U S A. 2003 Sep 2;100(18):10529-33. PMID: 12917492.
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