For research use only. Not for therapeutic Use.
R121919 (NBI30775) is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats[1][2][3].
R121919 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].
R121919 (NBI30775) 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 reduces levels of anxiety in mice with a steep dose-response curve[2].
| Catalog Number | R022288 |
| CAS Number | 195055-03-9 |
| Synonyms | 3-[6-(dimethylamino)-4-methylpyridin-3-yl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine |
| Molecular Formula | C22H32N6 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H32N6/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3/h12-14H,8-11H2,1-7H3 |
| InChIKey | ANNRUWYFVIGKHA-UHFFFAOYSA-N |
| SMILES | CCCN(CCC)C1=CC(=NC2=C(C(=NN12)C)C3=CN=C(C=C3C)N(C)C)C |
| Reference | [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. [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. [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. |
