AM-251 (drug)

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AM-251 (drug)

3D structure of AM-251
Another 3D view of AM-251

AM-251 is a chemical compound that acts as a selective antagonist of the cannabinoid receptor CB1. It is structurally related to the cannabinoid receptor antagonist rimonabant, and it is used primarily in scientific research to study the endocannabinoid system.

Chemical structure and properties

AM-251 is a member of the biarylpyrazole class of compounds. It has a complex chemical structure that includes a pyrazole ring, which is a five-membered ring containing three carbon atoms and two nitrogen atoms. The compound is characterized by its high affinity for the CB1 receptor, which is a G protein-coupled receptor located primarily in the central nervous system.

Mechanism of action

AM-251 functions as an inverse agonist at the CB1 receptor. This means that it binds to the receptor and induces a pharmacological response opposite to that of an agonist. By blocking the action of endogenous cannabinoids such as anandamide, AM-251 can modulate various physiological processes, including appetite, pain sensation, and mood.

Applications in research

AM-251 is widely used in preclinical studies to investigate the role of the CB1 receptor in various biological systems. It has been employed in studies related to obesity, addiction, and neurodegenerative diseases. Researchers use AM-251 to better understand the potential therapeutic applications of CB1 receptor modulation.

Safety and toxicity

As with many research chemicals, the safety profile of AM-251 is not fully established. It is primarily used in laboratory settings, and its effects in humans are not well-documented. Researchers handling AM-251 must follow appropriate safety protocols to minimize exposure and potential risks.

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AM-251 (drug)

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Contributors: Prab R. Tumpati, MD