CP 154,526 (hydrochloride)

CP 154,526 is an antagonist of corticotropin-releasing factor receptor 1 (CRF₁; K_i = 2.7 nM).^1,2 It is selective for CRF₁ over CRF₂ (K_i = >10 μM).¹ CP 154,526 inhibits CRF-induced increases in adrenocorticotropic hormone (ACTH) levels in rat plasma with an ID₅₀ value of 10 mg/kg. It increases the time spent in the open arms of the elevated plus maze in rats when administered at a dose of 1 mg/kg.³ CP 154,526 (10 mg/kg, twice per day for 14 days) decreases immobility time in the forced swim test in a rat model of depressive-like behavior.⁴ It also decreases stress-induced reinstatement of cocaine or heroin self-administration in cocaine- and heroin-trained rats, respectively, when administered at doses of 15 and 30 mg/kg.⁵

WARNING This product is not for human or veterinary use.

1. Schulz, D.W., Mansbach, R.S., Sprouse, J., et al. CP-154,526: A potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc. Natl. Acad. Sci. USA 93(19), 10477-10482 (1996).

2. Seymour, P.A., Schmidt, A.W., and Schulz, D.W. The pharmacology of CP-154,526, a non-peptide antagonist of the CRH1 receptor: A review. CNS Drug Rev. 9(1), 57-96 (2003).

3. Lundkvist, J., Chai, Z., Teheranian, R., et al. A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity. Eur. J. Pharmacol. 309(2), 195-200 (1996).

4. Overstreet, D.H., Keeney, A., and Hogg, S. Antidepressant effects of citalopram and CRF receptor antagonist CP-154,526 in a rat model of depression. Eur. J. Pharmacol. 492(2-3), 195-201 (2004).

5. Feng, S., Liu, D., Feng, W., et al. Allyl fluorescein ethers as promising fluorescent probes for carbon monoxide imaging in living cells. Anal. Chem. 89(6), 3754-3760 (2017).