Drug intelligence / Profile preview

CP-154,526

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal, Oral
01

Overview

CP-154,526 is a potent and selective non-peptide antagonist of the corticotropin-releasing hormone receptor 1 (CRF1), developed by Pfizer. It exhibits high affinity for CRF1 (Ki ≈ 2.7 nM) and is highly selective over CRF2 receptors. The compound readily penetrates the central nervous system following peripheral administration and blocks CRF-induced activation of adenylate cyclase as well as downstream neuroendocrine responses such as ACTH release. Preclinical studies have demonstrated anxiolytic-like activity in animal models, with potential therapeutic applications in conditions involving excessive CRF signaling such as anxiety disorders, depression, substance abuse (notably alcoholism), and stress-related pathologies[1][2][3][6][9].

Other names
CP 154526 hydrochlorideCP154526 hydrochlorideCP-154526 hydrochloride
02

Targets

CRHR1 (Corticotropin-releasing factor receptor 1)

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