Drug intelligence / Profile preview

AM1241

Development stage
Preclinical
Lead developer
Abbott
Modality
Small Molecules
Administration
Intraperitoneal (animals)
01

Overview

**AM1241** is a synthetic small molecule from the aminoalkylindole family developed as a highly potent and selective agonist for the cannabinoid receptor CB2. It shows an approximate Ki of 3.4 nM for CB2 with roughly 80-fold selectivity over the CB1 receptor, and it is widely used in research to study the physiological effects of CB2 activation. Mechanistically, AM1241 functions as a CB2 agonist, leading to analgesic and antihyperalgesic effects in animal models, particularly in conditions involving neuropathic or "atypical" pain such as hyperalgesia and allodynia. These effects are believed to be mediated through CB2-dependent peripheral release of endogenous opioid peptides, as well as direct activation of the TRPA1 channel. AM1241 has also shown some efficacy in animal models of diseases such as bone cancer pain and amyotrophic lateral sclerosis. It is used exclusively in research settings and is not approved for therapeutic use in humans[4][9][2][8].

Other names
(2-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole
02

Targets

CNR1 (Cannabinoid receptor 1)TRPA1 (Transient receptor potential cation channel subfamily A member 1)

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