R121919 hydrochloride  (Synonyms: NBI30775 hydrochloride)

R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a K_i of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats^[1][2][3].

R121919 hydrochloride is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

R121919 (NBI30775) hydrochloride dose dependently decreases adrenocorticopin hormone and Corticosterone (HY-B1618) responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively^[1].
R121919 hydrochloride reduces levels of anxiety in mice with a steep dose-response curve^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

416.99

C₂₂H₃₃ClN₆

195055-66-4

CCCN(CCC)C1=CC(C)=NC2=C(C3=C(C)C=C(N(C)C)N=C3)C(C)=NN12.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80.  [Content Brief]

  [2]. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.  [Content Brief]

  [3]. Gutman DA, et al. Behavioral effects of the CRF1 recepator antagonist R121919 in rats selectively bred for high and low activity in the swim test. Psychoneuroendocrinology. 2008 Sep;33(8):1093-101.  [Content Brief]