| Identification | Back Directory | [Name]
NBI 34041 | [CAS]
268545-87-5 | [Synonyms]
SB723620
SB-723620
NBI 34041
SB 723620
AKLMUGFDGONMAA-UHFFFAOYSA-N
6H-1,3,6,8a-Tetraazaacenaphthylene, 2-(2,4-dichlorophenyl)-7,8-dihydro-4-methyl-6-(1-propylbutyl)- | [Molecular Formula]
C22H26Cl2N4 | [MDL Number]
MFCD18782661 | [MOL File]
268545-87-5.mol | [Molecular Weight]
417.37 |
| Hazard Information | Back Directory | [Uses]
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research. | [in vivo]
NBI-34041 (3-30 mg/kg; oral gavage; a single dose) significantly attenuates the elevation in plasma ACTH induced by CRF. NBI-34041 also demonstrates efficacy in attenuating shock-induced ACTH release in a dose-dependent manner[1]. | Animal Model: | Male Wistar or Sprague-Dawley rats (300-350 g)[1] | | Dosage: | 3 mg/kg, 10 mg/kg, or 30 mg/kg | | Administration: | Oral gavage; a single dose | | Result: | Did not impair diurnal adrenocorticotropic hormone (ACTH) and cortisol secretion or CRF evoked ACTH and cortisol responses but attenuated the neuroendocrine response to psychosocial stress.
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| [IC 50]
CRFR1: 58.9 nM (IC50); CRFR1: 4 nM (Ki); CRFR2: >10000 nM (IC50) | [References]
[1] Marcus Ising, et al. High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response. Neuropsychopharmacology. 2007 Sep;32(9):1941-9. DOI:10.1038/sj.npp.1301328 |
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