R 121919 hydrochloride

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R 121919 hydrochloride | CAS No. 195055-66-4 | CRF1 Receptor Antagonists
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Description: High affinity CRF1 antagonist; orally bioavailable

Chemical Name: 3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine hydrochloride

Purity: ≥98%

Product Details

Biological Activity

R 121919 hydrochloride is a high affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable.

Technical Data

Soluble to 100 mM in ethanol and to 10 mM in DMSO with gentle warming
Store at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression.
    Chen and Grigoriadis
    Drug Dev.Res., 2005;65:216
  2. The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats.
    Jutkiewicz et al.
    Psychopharmacology (Berl)., 2005;180:215
  3. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress.
    Gutman et al.
    J.Pharmacol.Exp.Ther., 2003;304:874
  4. Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist.
    Heinrichs et al.
    Neuropsychopharmacology, 2002;27:194

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