Compounds > nbi-34041
Page last updated: 2024-11-11

nbi-34041

Description

NBI-34041: high-affinity CRF1 (corticotropin-releasing factor receptor 1) receptor antagonist for attenuating elevated stress response [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9888194
CHEMBL ID188907
SCHEMBL ID16606732
MeSH IDM0515983

Synonyms (19)

Synonym
CHEMBL188907 ,
bdbm50171325
2-(2,4-dichloro-phenyl)-4-methyl-6-(1-propyl-butyl)-7,8-dihydro-6h-1,3,6,8a-tetraaza-acenaphthylene
nbi-34041
1-(2,4-dichlorophenyl)-5-(heptan-4-yl)-7-methyl-4,5-dihydro-3h-2,2a,5,8-tetraazaacenaphthylene
874OEY3JEJ ,
sb723620
sb-723620
6h-1,3,6,8a-tetraazaacenaphthylene, 2-(2,4-dichlorophenyl)-7,8-dihydro-4-methyl-6-(1-propylbutyl)-
268545-87-5
SCHEMBL16606732
unii-874oey3jej
3-(2,4-dichlorophenyl)-9-heptan-4-yl-6-methyl-1,2,5,9-tetrazatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraene
nbi 34041
Q27269794
compound 16a [pmid: 16078829]
nbi34041
gtpl10375
AKOS040753222

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" These results suggest that NBI-34041 is safe and does not impair basal regulation of the HPA system but improves resistance against psychosocial stress."( High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response.
Foster, AC; Grigoriadis, DE; Holsboer, F; Ising, M; Künzel, HE; Learned-Coughlin, SM; Uhr, M; Zimmermann, US, 2007)		0.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Corticotropin-releasing factor receptor 1Homo sapiens (human)Ki0.00450.00080.01020.2400AID239687; AID254614; AID609182
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
immune responseCorticotropin-releasing factor receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
activation of adenylate cyclase activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
female pregnancyCorticotropin-releasing factor receptor 1Homo sapiens (human)
parturitionCorticotropin-releasing factor receptor 1Homo sapiens (human)
regulation of adenylate cyclase activity involved in G protein-coupled receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
adrenal gland developmentCorticotropin-releasing factor receptor 1Homo sapiens (human)
exploration behaviorCorticotropin-releasing factor receptor 1Homo sapiens (human)
fear responseCorticotropin-releasing factor receptor 1Homo sapiens (human)
behavioral response to ethanolCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin secretionCorticotropin-releasing factor receptor 1Homo sapiens (human)
general adaptation syndrome, behavioral processCorticotropin-releasing factor receptor 1Homo sapiens (human)
cellular response to corticotropin-releasing hormone stimulusCorticotropin-releasing factor receptor 1Homo sapiens (human)
negative regulation of voltage-gated calcium channel activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
regulation of corticosterone secretionCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
protein bindingCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotrophin-releasing factor receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin-releasing hormone bindingCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin-releasing hormone receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endosomeCorticotropin-releasing factor receptor 1Homo sapiens (human)
plasma membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
plasma membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
neuron projectionCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID609182Antagonist activity at human CRF-1 receptor2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
AID254614Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
AID239687Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (60.00)29.6817
2010's2 (40.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (20.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
nbi 27914
[no description available]		2.0610dialkylarylamine;
tertiary amino compound
antalarmin
antalarmin : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidin-4-amine which is substituted by methyl groups at positions 2, 5, and 6, by a mesityl group at position 7, and in which the amino substituent at position 4 has been substituted by ethyl and butyl groups. It is an antagonist of corticotropin-releasing factor 1 (CRF-1) receptors (Ki = 1 nM).		2.4320pyrrolopyrimidine;
tertiary amino compound		corticotropin-releasing factor receptor antagonist
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		3.1510heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
cp 154526
[no description available]		2.4420
r 121919
[no description available]		2.4420
pexacerfont
[no description available]		2.0610pyrazolopyridine
dmp 696
DMP 696: a CRF(1) receptor antagonist; structure in first source		2.4420
atrial natriuretic factor
Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.		3.1510polypeptide
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		3.1510(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
ConditionIndicatedRelationship StrengthStudiesTrials
Anxiety Neuroses
[description not available]		02.9710
Anxiety Disorders
Persistent and disabling ANXIETY.		02.9710
chemdatabank.com