CP-154,526

CP-154,526 is a non-peptide antagonist of corticotropin-releasing hormone receptor 1 (CRHR1). It was developed by Pfizer in the 1990s and has been used in scientific research to study the role of CRHR1 in stress, anxiety, depression, and other conditions.

Chemistry

CP-154,526 is a small molecule that binds to CRHR1, blocking its interaction with corticotropin-releasing hormone (CRH). Its chemical structure is distinct from that of peptide-based CRHR1 antagonists, which allows it to have different pharmacokinetic properties and potentially broader applications.

Pharmacology

CP-154,526 acts as a selective antagonist at CRHR1, meaning it prevents the activation of this receptor by its natural ligand, CRH. By blocking CRHR1, CP-154,526 can modulate the body's response to stress and potentially influence behavior and mood.

Research

CP-154,526 has been used in a variety of preclinical studies to investigate the role of CRHR1 in stress response, anxiety, and depression. For example, it has been shown to reduce anxiety-like behavior in animal models of stress. It has also been used to study the role of CRHR1 in alcohol dependence, as CRHR1 has been implicated in the stress-related aspects of this condition.

Potential Therapeutic Uses

While CP-154,526 is not currently approved for any therapeutic uses, research suggests that CRHR1 antagonists like CP-154,526 could potentially be used to treat a variety of conditions, including anxiety disorders, depression, and alcohol dependence. However, more research is needed to fully understand the potential benefits and risks of this approach.

See Also

• Corticotropin-releasing hormone receptor
• Corticotropin-releasing hormone
• Pfizer

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