Zevaquenabant

A cannabinoid receptor type 1 antagonist

Zevaquenabant
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CAS Number	870054-44-9
PubChem	11523733
DrugBank
ChemSpider	9700915
KEGG	D09992

Zevaquenabant is a cannabinoid receptor type 1 (CB1) antagonist that was developed for potential use in the treatment of obesity and related metabolic disorders. It is a member of the class of compounds known as cannabinoid receptor antagonists, which are designed to block the effects of endocannabinoids and cannabinoid drugs.

Mechanism of Action

Zevaquenabant functions by selectively binding to the CB1 receptor, which is primarily located in the central nervous system and peripheral tissues. By blocking this receptor, zevaquenabant inhibits the action of endocannabinoids, which are involved in the regulation of appetite, energy balance, and lipid metabolism. This mechanism is similar to that of other CB1 antagonists, such as rimonabant.

Development and Clinical Trials

Zevaquenabant was developed by Pfizer as part of their research into treatments for obesity. However, like many other CB1 antagonists, its development was halted due to concerns about psychiatric side effects, including depression and anxiety. These side effects are thought to result from the blockade of CB1 receptors in the brain, which can affect mood and behavior.

Pharmacokinetics

The pharmacokinetic profile of zevaquenabant includes its absorption, distribution, metabolism, and excretion. As a lipophilic compound, it is expected to have good absorption and distribution in fatty tissues. The metabolism of zevaquenabant likely involves hepatic enzymes, and its excretion is primarily through the renal and biliary systems.

Potential Applications

While zevaquenabant was primarily investigated for the treatment of obesity, CB1 antagonists have also been explored for other potential applications, including the treatment of addiction, metabolic syndrome, and type 2 diabetes. However, the psychiatric side effects have limited their clinical use.

Related Pages

• Cannabinoid receptor type 1
• Endocannabinoid system
• Rimonabant
• Obesity
• Metabolic syndrome