| Identification | Back Directory | [Name]
3-(6-(DIMETHYLAMINO)-4-METHYLPYRIDIN-3-YL)-2,5-DIMETHYL-N,N-DIPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-AMINE HYDROCHLORIDE | [CAS]
195055-66-4 | [Synonyms]
R 121919 hydrochloride
R121919 (NBI-30775) Hydrochloride
3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine hydrochloride
3-(6-(DIMETHYLAMINO)-4-METHYLPYRIDIN-3-YL)-2,5-DIMETHYL-N,N-DIPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-AMINE HYDROCHLORIDE | [Molecular Formula]
C22H33ClN6 | [MDL Number]
MFCD13152289 | [MOL File]
195055-66-4.mol | [Molecular Weight]
417 |
| Hazard Information | Back Directory | [Uses]
R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats[1][2][3]. | [in vivo]
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]. | [IC 50]
CRFR1: 2-5 nM (Ki) | [storage]
Store at +4°C | [References]
[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. DOI:10.1124/jpet.102.042788
[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. DOI:10.1007/s00213-004-2134-x
[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. DOI:10.1016/j.psyneuen.2008.05.003 |
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