Compounds > nnc 38-1049
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nnc 38-1049

Description

NNC 38-1049: selective histamine H3 receptor antagonist; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID9798429
CHEMBL ID97170
SCHEMBL ID4386760
MeSH IDM0498715

Synonyms (22)

Synonym
CHEMBL97170 ,
L023140
bdbm50146835
1-(4-chloro-phenyl)-4-(4-cyclopentyl-piperazin-1-yl)-butane-1,4-dione; hydrochloride
1-(4-chlorophenyl)-4-(4-cyclopentylpiperazin-1-yl)butane-1,4-dione
piperazine, 1-[4-(4-chlorophenyl)-1,4-dioxobutyl]-4-cyclopentyl-
nnc 38-1049
757183-18-9
SCHEMBL4386760
1-(4-chlorophenyl)-4-(4-cyclopentyl-1-piperazinyl)-1,4-butanedione
DTXSID70430911
1-(4-chlorophenyl)-4-(4-cyclopentylpiperazine-1-yl)-4-oxobutan-1-one
nnc-38-1049
Q6593955
nn 0038-0000-1049
piperazine, 1-(4-(4-chlorophenyl)-1,4-dioxobutyl)-4-cyclopentyl-
ncc-0028-1049
unii-63g6tld54v
63g6tld54v ,
1,4-butanedione, 1-(4-chlorophenyl)-4-(4-cyclopentyl-1-piperazinyl)-
AKOS040749034
Z375463996

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Histamine H3 receptorHomo sapiens (human)Ki0.0012AID1729009; AID599203; AID692494

Bioassays (4)

Assay IDTitleYearJournalArticle
AID692494Binding affinity to human histamine H3 receptor2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
ISSN: 1520-4804		Histamine H3 receptor as a drug discovery target.
AID599205Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
ISSN: 1768-3254		Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
AID599203Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
ISSN: 1768-3254		Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
AID1729009Binding affinity to human H3R2021European journal of medicinal chemistry, Mar-05, Volume: 213ISSN: 1768-3254Structural modifications in the distal, regulatory region of histamine H

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's1 (20.00)24.3611
2020's1 (20.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
clobenpropit
1
imidazoles;
imidothiocarbamic ester;
organochlorine compound		H3-receptor antagonist;
H4-receptor agonist		202120213.0low000001
imetit
1
imidazoles;
imidothiocarbamic ester		H3-receptor agonist;
H4-receptor agonist		2011201113.0low000010
sr141716
1
amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist		202120213.0low000001
alpha-methylhistamine
1
aralkylamino compound;
imidazoles		H3-receptor agonist2009200915.0low000100
interferon-gamma
1
2009200915.0medium000100
jnj-5207852
3
2009202110.3high000111
4-(1h-imidazol-4-ylmethyl)piperidine
1
piperidines2011201113.0low000010
thioperamide
3
primary aliphatic amine2009202110.3medium000111
ciproxifan
1
aromatic ketone202120213.0low000001
gt 2331
1
2011201113.0medium000010
dibutyl phthalate
1
2011201113.0low000010
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)-
2
2009201114.0medium000110
a 304121
1
2011201113.0medium000010
jnj 10181457
1
2009200915.0medium000100
pitolisant
2
organochlorine compound200920219.0low000101
a 317920
1
2011201113.0medium000010
pf 03654746
1
2011201113.0high000010
gsk 1004723
1
2011201113.0medium000010
clozapine
1
benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic		2011201113.0low000010
olanzapine
1
benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor		2011201113.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
histamine
1
aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter		2006200618.0low000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Body Weight0
3
2005202113.3high000201
Obesity0
1
2006200618.0medium000100
Weight Loss0
1
2006200618.0medium000100
Weight Reduction0
1
2006200618.0medium000100

Dosage (2)

ArticleYear
Increase of neuronal histamine in obese rats is associated with decreases in body weight and plasma triglycerides.
Obesity (Silver Spring, Md.), , Volume: 14, Issue:12		2006
Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and body weight.
International journal of obesity (2005), , Volume: 29, Issue:12		2005