Pexacerfont

Pexacerfont is an antagonist of corticotropin-releasing factor receptor 1 (CRF₁; IC₅₀ = 6.1 nM for the human receptor).¹ It is selective for CRF₁ in IMR-32 cells (mean IC₅₀ = 10.6 nM) over CFR_2β receptors endogenously expressed in pig choroid plexus membranes (IC₅₀ = >1,000 nM) in radioligand binding assays and does not bind to the human CRF binding protein (IC₅₀ = >1,000 nM). Pexacerfont inhibits adrenocorticotropic hormone (ACTH) release induced by CRF in primary rat pituitary cells with an IC₅₀ value of 129 nM. It increases the time spent in the open arms of the elevated plus maze (EPM) in rats, indicating anxiolytic-like activity, when administered at doses ranging from 10 to 30 mg/kg.

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1. Gilligan, P.J., Clarke, T., He, L., et al. Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: Potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. J. Med. Chem. 52(9), 3084-3092 (2009).