NBI-30775
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MedKoo CAT#: 522653

CAS#: 195055-03-9

Description: NBI-30775, also known as R121919, is a CRF1 receptor antagonist. R121919 attenuates the severity of precipitated morphine. Treatment with R121919 improves sleep-EEG in patients with depression. R121919 attenuates stress-elicited sleep disturbances in rats, particularly in those with high innate anxiety.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 450 Inquiry
50mg USD 1150 Inquiry
Inquire bulk and customized quantity

Pricing updated 2020-02-17. Prices are subject to change without notice.

NBI-30775, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 522653
Name: NBI-30775
CAS#: 195055-03-9
Chemical Formula: C22H32N6
Exact Mass: 380.2688
Molecular Weight: 380.54
Elemental Analysis: C, 69.44; H, 8.48; N, 22.08


Synonym: R121919; R-121919; R 121919; R121,919; R-121,919; R 121,919; NBI30775; NBI 30775; NBI-30775

IUPAC/Chemical Name: 3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine

InChi Key: ANNRUWYFVIGKHA-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: CCCN(CCC)C1=CC(C)=NC2=C(C3=C(C)C=C(N(C)C)N=C3)C(C)=NN12


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934990300


References

1: Hanson ND, Nemeroff CB, Owens MJ. Lithium, but not fluoxetine or the corticotropin-releasing factor receptor 1 receptor antagonist R121919, increases cell proliferation in the adult dentate gyrus. J Pharmacol Exp Ther. 2011 Apr;337(1):180-6. doi: 10.1124/jpet.110.175372. Epub 2011 Jan 10. PubMed PMID: 21220416; PubMed Central PMCID: PMC3063735.

2: Gutman DA, Owens MJ, Thrivikraman KV, Nemeroff CB. Persistent anxiolytic affects after chronic administration of the CRF₁ receptor antagonist R121919 in rats. Neuropharmacology. 2011 Jun;60(7-8):1135-41. doi: 10.1016/j.neuropharm.2010.10.004. Epub 2010 Oct 14. PubMed PMID: 20951149; PubMed Central PMCID: PMC3079005.

3: Gutman DA, Coyer MJ, Boss-Williams KA, Owens MJ, Nemeroff CB, Weiss JM. Behavioral effects of the CRF1 receptor 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. Epub 2008 Aug 3. Erratum in: Psychoneuroendocrinology. 2009 May;34(4):630-1. PubMed PMID: 18676086.

4: Erhardt A, Müller MB, Rödel A, Welt T, Ohl F, Holsboer F, Keck ME. Consequences of chronic social stress on behaviour and vasopressin gene expression in the PVN of DBA/2OlaHsd mice--influence of treatment with the CRHR1-antagonist R121919/NBI 30775. J Psychopharmacol. 2009 Jan;23(1):31-9. doi: 10.1177/0269881108089813. Epub 2008 May 30. PubMed PMID: 18515457.

5: Skelton KH, Oren D, Gutman DA, Easterling K, Holtzman SG, Nemeroff CB, Owens MJ. The CRF1 receptor antagonist, R121919, attenuates the severity of precipitated morphine withdrawal. Eur J Pharmacol. 2007 Sep 24;571(1):17-24. Epub 2007 Jun 5. PubMed PMID: 17610870.

6: Skelton KH, Gutman DA, Thrivikraman KV, Nemeroff CB, Owens MJ. The CRF1 receptor antagonist R121919 attenuates the neuroendocrine and behavioral effects of precipitated lorazepam withdrawal. Psychopharmacology (Berl). 2007 Jun;192(3):385-96. Epub 2007 Feb 13. PubMed PMID: 17297634.

7: Jutkiewicz EM, Wood SK, Houshyar H, Hsin LW, Rice KC, Woods JH. 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. Psychopharmacology (Berl). 2005 Jul;180(2):215-23. Epub 2005 Feb 5. PubMed PMID: 15696320; PubMed Central PMCID: PMC1315297.

8: Post A, Ohl F, Almeida OF, Binder EB, Rücker M, Welt S, Binder E, Holsboer F, Sillaber I. 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. Epub 2005 Jan 29. PubMed PMID: 15682302.

9: Künzel HE, Ising M, Zobel AW, Nickel T, Ackl N, Sonntag A, Holsboer F, Uhr M. Treatment with a CRH-1-receptor antagonist (R121919) does not affect weight or plasma leptin concentration in patients with major depression. J Psychiatr Res. 2005 Mar;39(2):173-7. PubMed PMID: 15589565.

10: Chen C, Wilcoxen KM, Huang CQ, Xie YF, McCarthy JR, Webb TR, Zhu YF, Saunders J, Liu XJ, Chen TK, Bozigian H, Grigoriadis DE. Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]py rimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists. J Med Chem. 2004 Sep 9;47(19):4787-98. PubMed PMID: 15341493.

11: Held K, Künzel H, Ising M, Schmid DA, Zobel A, Murck H, Holsboer F, Steiger A. Treatment with the CRH1-receptor-antagonist R121919 improves sleep-EEG in patients with depression. J Psychiatr Res. 2004 Mar-Apr;38(2):129-36. PubMed PMID: 14757326.

12: Künzel HE, Zobel AW, Nickel T, Ackl N, Uhr M, Sonntag A, Ising M, Holsboer F. Treatment of depression with the CRH-1-receptor antagonist R121919: endocrine changes and side effects. J Psychiatr Res. 2003 Nov-Dec;37(6):525-33. PubMed PMID: 14563384.

13: Keck ME, Welt T, Müller MB, Landgraf R, Holsboer F. The high-affinity non-peptide CRH1 receptor antagonist R121919 attenuates stress-induced alterations in plasma oxytocin, prolactin, and testosterone secretion in rats. Pharmacopsychiatry. 2003 Jan;36(1):27-31. PubMed PMID: 12649771.

14: Gutman DA, Owens MJ, Skelton KH, Thrivikraman KV, Nemeroff CB. 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. PubMed PMID: 12538845.

15: Lancel M, Müller-Preuss P, Wigger A, Landgraf R, Holsboer F. The CRH1 receptor antagonist R121919 attenuates stress-elicited sleep disturbances in rats, particularly in those with high innate anxiety. J Psychiatr Res. 2002 Jul-Aug;36(4):197-208. PubMed PMID: 12191624.

16: Keck ME, Welt T, Wigger A, Renner U, Engelmann M, Holsboer F, Landgraf R. The anxiolytic effect of the CRH(1) receptor antagonist R121919 depends on innate emotionality in rats. Eur J Neurosci. 2001 Jan;13(2):373-80. PubMed PMID: 11168542.

17: Zobel AW, Nickel T, Künzel HE, Ackl N, Sonntag A, Ising M, Holsboer F. Effects of the high-affinity corticotropin-releasing hormone receptor 1 antagonist R121919 in major depression: the first 20 patients treated. J Psychiatr Res. 2000 May-Jun;34(3):171-81. PubMed PMID: 10867111.