NBI-34041

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H26Cl2N4
Molecular Weight	417.375
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCCC(CCC)N1CCN2N=C(C3=C2C1=CC(C)=N3)C4=CC=C(Cl)C=C4Cl

InChI

InChIKey=AKLMUGFDGONMAA-UHFFFAOYSA-N

InChI=1S/C22H26Cl2N4/c1-4-6-16(7-5-2)27-10-11-28-22-19(27)12-14(3)25-21(22)20(26-28)17-9-8-15(23)13-18(17)24/h8-9,12-13,16H,4-7,10-11H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C22H26Cl2N4
Molecular Weight	417.375
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Substance Class	Chemical
Record UNII	874OEY3JEJ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SB-723620

Preferred Name

English

NBI-34041

Common Name

English

1-(2,4-DICHLOROPHENYL)-5-(HEPTAN-4-YL)-7-METHYL-4,5-DIHYDRO-3H-2,2A,5,8-TETRAAZAACENAPHTHYLENE

Systematic Name

English

SB723620

Code

English

6H-1,3,6,8A-TETRAAZAACENAPHTHYLENE, 2-(2,4-DICHLOROPHENYL)-7,8-DIHYDRO-4-METHYL-6-(1-PROPYLBUTYL)-

Systematic Name

English

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Code System

Code

Type

Description

FDA UNII

874OEY3JEJ

PRIMARY

CAS

268545-87-5

PRIMARY

PUBCHEM

9888194

PRIMARY

MANUFACTURER PRODUCT INFORMATION

NBI-34041

PRIMARY

Description: NBI-34041 is potent and high-affinity CRF1 receptor antagonist. NBI-34041 is safety and efficacy in attenuating elevated stress response. NBI-34041 is effective in reducing endocrine responses to pharmacological and behavioral challenge mediated by CRF(1) receptors. NBI-34041 is safe and does not impair basal regulation of the HPA system but improves resistance against psychosocial stress. NBI-34041 demonstrates that inhibition of the CRF system is a promising target for drug development against depression and anxiety disorders. (last updated: 3/8/2016).

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Related Record

Type

Details


					874OEY3JEJ

NBI-34041

ACTIVE MOIETY

Comments:

Developer: GlaxoSmithKline; Class: Acenaphthene, Antidepressant, Antispasmodic, Anxiolytic, Irritable bowel syndrome therapy; Mechanism of Action: Corticotropin-releasing factor antagonists; Highest Development Phase: Discontinued for Anxiety disorders, Irritable bowel syndrome and Major depressive disorder


					874OEY3JEJ

NBI-34041

ACTIVE MOIETY

Comments:

These specific properties and its well-documented safety profile enabled a clinical Phase I study with 24 healthy male subjects receiving NBI-34041 (10, 50, or 100 mg) or placebo for 14 days. Regulation of the hypothalamic-pituitary-adrenocortical (HPA) axis was evaluated by intravenous stimulation with 100 mg of human CRF. Treatment with NBI-34041 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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