Drug intelligence / Profile preview

CP-376395

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

Overview

CP-376395 is a potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist that binds at an allosteric site on the receptor. It displays high selectivity for CRF1 over CRF2, with reported Ki values of 12 nM for CRF1 and greater than 10,000 nM for CRF2. The compound inhibits CRF-induced activation of the hypothalamic-pituitary-adrenal (HPA) axis in vivo and is orally active. Mechanistically, CP-376395 may attenuate stress and stress-related behaviors, and has been studied for its effects on ethanol drinking in animal models relevant to alcohol use disorder and post-traumatic stress disorder. Its chemical name is N-(1-ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinamine hydrochloride[1][4][8][10].

Other names
CP-376395 hydrochlorideCP376395 hydrochlorideCP 376395 hydrochloride
02

Targets

CRHR1 (Corticotropin-releasing factor receptor 1)

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