R121919，5MG，SML3114-5MG，Sigma

Biochem/physiol Actions

Brain-penetrant and orally available selective CRF1 (CRFR-1, CRHR-1) antagonist with in vivo antistress efficacy.
R121919 (NBI 30775) is a brain-penetrant, orally available high-affinity corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) antagonist (Ki = 3.5 nM against sauvagine for binding hCRFR1-expressing HEK293 cells; IC50 = 20 nM/CRF-stimulated ACTH release from rat anterior pituitary cells & IC50 = 80 nM/CRF-stimulated cAMP production in hCRFR1-expressing HEK293 cells) without affinity toward CRFR2. In addition to its antistress efficacy in various rat anxiety models (0.63-20 mg/kg p.o.), R121919 also demonstrates therapeutic efficacy and long-term safety in Alzheimer′s disease (AD) mice (20 mg/kg/day s.c.) in vivo.