AM281

Overview

AM281 is a synthetic compound that acts as a selective antagonist of the cannabinoid receptor CB1. It is structurally related to other cannabinoid receptor antagonists and is used primarily in research settings to study the endocannabinoid system and its physiological roles.

Chemical Structure and Properties

AM281 is a member of the biarylpyrazole class of compounds. Its chemical structure is characterized by a pyrazole ring linked to a biaryl moiety, which is crucial for its activity as a CB1 receptor antagonist. The compound's IUPAC name is N-(morpholin-4-yl)-1-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide.

Mechanism of Action

AM281 functions by binding to the CB1 receptor, which is a G protein-coupled receptor predominantly found in the central nervous system. By acting as an antagonist, AM281 inhibits the action of endogenous cannabinoids such as anandamide and 2-arachidonoylglycerol (2-AG), thereby modulating various physiological processes including pain perception, appetite, and mood.

Research Applications

AM281 is widely used in preclinical research to explore the role of the endocannabinoid system in various physiological and pathological processes. Studies have utilized AM281 to investigate:

• The modulation of pain and analgesia
• The regulation of appetite and metabolism
• The effects on memory and cognition
• The potential therapeutic applications in neurodegenerative diseases

Pharmacokinetics

The pharmacokinetic profile of AM281 includes its absorption, distribution, metabolism, and excretion. As a research compound, detailed pharmacokinetic data may vary depending on the experimental model used. Typically, AM281 is administered in laboratory settings via intraperitoneal or intravenous routes.

Safety and Toxicology

As with many research chemicals, the safety profile of AM281 is not fully established for human use. In animal studies, it is important to monitor for any adverse effects, particularly those related to the central nervous system, given its action on CB1 receptors.

Also see

• Cannabinoid receptor
• CB1 receptor
• Endocannabinoid system
• Cannabinoid receptor antagonist
• Anandamide
• 2-arachidonoylglycerol