R-121,919
R-121,919 Basic information
- Product Name:
- R-121,919
- Synonyms:
-
- NBI30775;R 121919;R-121919
- R-121,919
- 3-(6-(DIMETHYLAMINO)-4-METHYLPYRIDIN-3-YL)-2,5-DIMETHYL-N,N-DIPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-AMINE
- NBI 30775
- 3-[6-(diMethylaMino)-4-Methyl-3-pyridinyl]-2,5-diMethyl-N,N-dipropyl-pyrazolo[2,3-a]pyriMidine-7-aMine
- 3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-am
- 3-[6-(DiMethylaMino)-4-Methyl-3-pyridinyl]-2,5-diMethyl-N,N-dipropylpyrazolo[1,5-a]pyriMidin-7-aMine
- -2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
- CAS:
- 195055-03-9
- MF:
- C22H32N6
- MW:
- 380.53
- Mol File:
- 195055-03-9.mol
R-121,919 Chemical Properties
- Density
- 1.11±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 6.2 mg/mL (16.29 mM)
- form
- Solid
- pka
- 6.33±0.10(Predicted)
- color
- White to off-white
- 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(C)=NC2=C(C(C)=NN12)C3=CN=C(C=C3C)N(C)C
R-121,919 Usage And Synthesis
Uses
3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine, is a potent and Orally active Corticotropin-Releasing factor 1 receptor antagonists, which is hown to reduce negative emotional symptoms of acute and protracted alcohol withdrawal, and thus used for the treatment of alcoholism.
Biological Activity
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 r at 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 r at anxiety models (0.63-20 mg/kg p.o.), R121919 also demonstrates therapeutic efficacy and long-term safety in Alzheimerμs disease (AD) mice (20 mg/kg/day s.c.) in vivo.
in vivo
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].
IC 50
CRFR1: 2-5 nM (Ki)
R-121,919Supplier
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