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Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
ChEMBL | |
ECHA InfoCard | 100.164.689 |
Chemical and physical data | |
Formula | C22H22IN3O3 |
Molar mass | 503.340 g·mol−1 |
3D model ( JSmol) | |
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(what is this?) (verify) |
AM-1241 (1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole) is a chemical from the aminoalkylindole family that acts as a potent and selective agonist for the cannabinoid receptor CB2, [1] [2] with a Ki of 3.4 nM at CB2 and 80 times selectivity over the related CB1 receptor. [3] [4] It has analgesic effects in animal studies, particularly against "atypical" pain such as hyperalgesia and allodynia. [5] This is thought to be mediated through CB2-mediated peripheral release of endogenous opioid peptides, [6] as well as direct activation of the TRPA1 channel. [7] It has also shown efficacy in the treatment of amyotrophic lateral sclerosis in animal models. [8] [9]
The antihyperalgesic effects of AM-1241 were investigated in a murine 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 antagonist SR-144,528 reversed the acute effects of AM-1241 on both spontaneous and evoked pain, while having no effect on its own. [10]
Legal status | |
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Legal status |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
ChEMBL | |
ECHA InfoCard | 100.164.689 |
Chemical and physical data | |
Formula | C22H22IN3O3 |
Molar mass | 503.340 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(what is this?) (verify) |
AM-1241 (1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole) is a chemical from the aminoalkylindole family that acts as a potent and selective agonist for the cannabinoid receptor CB2, [1] [2] with a Ki of 3.4 nM at CB2 and 80 times selectivity over the related CB1 receptor. [3] [4] It has analgesic effects in animal studies, particularly against "atypical" pain such as hyperalgesia and allodynia. [5] This is thought to be mediated through CB2-mediated peripheral release of endogenous opioid peptides, [6] as well as direct activation of the TRPA1 channel. [7] It has also shown efficacy in the treatment of amyotrophic lateral sclerosis in animal models. [8] [9]
The antihyperalgesic effects of AM-1241 were investigated in a murine 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 antagonist SR-144,528 reversed the acute effects of AM-1241 on both spontaneous and evoked pain, while having no effect on its own. [10]