AM-4113

= AM-4113 =

AM-4113 is a chemical compound that acts as a selective antagonist of the cannabinoid receptor CB1. It is structurally related to other cannabinoid receptor antagonists, such as rimonabant, but has distinct pharmacological properties.

Chemical Structure and Properties

AM-4113 is a synthetic compound with the IUPAC name 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide. Its molecular formula is C21H20BrCl2N3O, and it has a molecular weight of 481.21 g/mol.

The compound is characterized by a pyrazole core, which is a common feature in many cannabinoid receptor ligands. The presence of halogen atoms, such as bromine and chlorine, contributes to its binding affinity and selectivity for the CB1 receptor.

Mechanism of Action

AM-4113 functions as a CB1 receptor antagonist. The CB1 receptor is a G protein-coupled receptor (GPCR) that is primarily found in the central nervous system, where it mediates the effects of endogenous cannabinoids like anandamide and 2-arachidonoylglycerol (2-AG), as well as exogenous cannabinoids such as THC from cannabis.

By blocking the CB1 receptor, AM-4113 inhibits the action of these cannabinoids, which can lead to a variety of physiological effects. Unlike CB1 receptor agonists, which can produce psychoactive effects, antagonists like AM-4113 are being studied for their potential to modulate appetite, pain, and other processes without causing psychoactivity.

Pharmacological Effects

Research on AM-4113 has primarily focused on its potential as an anti-obesity agent. By antagonizing the CB1 receptor, AM-4113 may reduce appetite and food intake, which could be beneficial in the treatment of obesity and related metabolic disorders.

In preclinical studies, AM-4113 has been shown to decrease food consumption in animal models without producing the adverse psychiatric effects associated with some other CB1 antagonists, such as rimonabant. This suggests that AM-4113 may have a more favorable side effect profile.

Clinical Development and Research

As of the latest updates, AM-4113 has not been approved for clinical use, and its development is primarily in the research phase. Studies continue to explore its efficacy and safety in various models, with a focus on its potential therapeutic applications in obesity and metabolic syndrome.

Conclusion

AM-4113 represents a promising compound in the field of cannabinoid receptor research. Its selective antagonism of the CB1 receptor offers potential therapeutic benefits, particularly in the management of obesity, without the psychoactive effects associated with cannabinoid receptor agonists. Ongoing research will further elucidate its clinical potential and safety profile.

References

• Pertwee, R. G. (2006). Cannabinoid pharmacology: the first 66 years. British Journal of Pharmacology, 147(S1), S163-S171.
• Di Marzo, V., & Matias, I. (2005). Endocannabinoid control of food intake and energy balance. Nature Neuroscience, 8(5), 585-589.
• Cota, D., & Woods, S. C. (2005). The role of the endocannabinoid system in the regulation of energy homeostasis. Current Opinion in Endocrinology, Diabetes, and Obesity, 12(4), 338-351.