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| ECHA InfoCard | 100.164.689 |
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| Formula | C22H22IN3O3 |
| Molar mass | 503.340 g·mol−1 |
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AM-1241 (1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole) is a chemical from theaminoalkylindole family that acts as a potent and selectiveagonist for thecannabinoid receptorCB2,[1][2] with aKi of 3.4 nM at CB2 and 80 times selectivity over the relatedCB1 receptor.[3][4] It hasanalgesic effects in animal studies, particularly against "atypical" pain such ashyperalgesia andallodynia.[5] This is thought to be mediated through CB2-mediated peripheral release of endogenousopioid peptides,[6] as well as direct activation of theTRPA1 channel.[7] It has also shown efficacy in the treatment ofamyotrophic lateral sclerosis in animal models.[8][9]
The antihyperalgesic effects of AM-1241 were investigated in amurine bone cancer model.Sarcoma cells were injected into the femur of a mouse, and then mice were injected twice daily with AM-1241. Treatment with AM-1241 reduced both spontaneous and evoked pain, as well as reducing the bone loss and subsequent fractures due to the tumor. Pretreatment with the CB2 antagonistSR-144,528 reversed the acute effects of AM-1241 on both spontaneous and evoked pain, while having no effect on its own.[10]