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Details

Stereochemistry ACHIRAL
Molecular Formula C14H17ClN4S
Molecular Weight 308.83
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOBENPROPIT

SMILES

ClC1=CC=C(CNC(=N)SCCCC2=CN=CN2)C=C1

InChI

InChIKey=UCAIEVHKDLMIFL-UHFFFAOYSA-N
InChI=1S/C14H17ClN4S/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19)

HIDE SMILES / InChI

Molecular Formula C14H17ClN4S
Molecular Weight 308.83
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.0 nM [IC50]
PubMed

PubMed

TitleDatePubMed
Effects of histamine H3 receptor agonists and antagonists on cognitive performance and scopolamine-induced amnesia.
1999 Oct
Identification of a histamine H(3)-like receptor in the zebrafish (Danio rerio) brain.
2000 Aug
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
2000 Dec
Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
2000 Jun
Genomic organization and characterization of splice variants of the human histamine H3 receptor.
2001 Apr 15
Histaminergic modulation of GABAergic transmission in rat ventromedial hypothalamic neurones.
2001 Aug 1
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
2001 Dec
H3 receptor-mediated inhibition of intestinal acetylcholine release: pharmacological characterization of signal transduction pathways.
2001 Feb
Cortical acetylcholine release elicited by stimulation of histamine H1 receptors in the nucleus basalis magnocellularis: a dual-probe microdialysis study in the freely moving rat.
2001 Jan
The rat H3 receptor: gene organization and multiple isoforms.
2001 Jan 12
[Identification and characterization of histamine H4 receptor].
2001 Jul
Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists.
2001 Jun
Cloning and characterization of a novel human histamine receptor.
2001 Mar
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
2001 Mar
[Role of central histamine in amygdaloid kindled seizures].
2001 May
Dynamics of histamine H(3) receptor antagonists on brain histamine metabolism: do all histamine H(3) receptor antagonists act at a single site?
2001 Nov 16
Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
2001 Oct
Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model.
2002 Jun
Activation of the extraneuronal monoamine transporter (EMT) from rat expressed in 293 cells.
2002 Nov
Ligands for histamine H(3) receptors modulate cell proliferation and migration in rat oxyntic mucosa.
2002 Sep
Replacement of imidazole by a piperidine moiety differentially affects the potency of histamine H3-receptor antagonists.
2003 Jan
Histamine induces cytoskeletal changes in human eosinophils via the H(4) receptor.
2003 Nov
Effects of endogenous histamine on seizure development of pentylenetetrazole-induced kindling in rats.
2003 Sep
Histamine H3 receptor activation inhibits dopamine D1 receptor-induced cAMP accumulation in rat striatal slices.
2004 Jul 8
[Mechanisms of the effect of brain histamine on chronic epilepsy induced by pentylenetetrazole].
2004 May
Effect of the histamine H3-antagonist clobenpropit on spatial memory deficits induced by MK-801 as evaluated by radial maze in Sprague-Dawley rats.
2004 May 5
Histamine (H3) receptors modulate the excitatory amino acid receptor response of the vestibular afferents.
2005 Dec 7
Histamine-3 receptor antagonists reduce superoxide anion generation and lipid peroxidation in rat brain homogenates.
2005 Jun
Influence of intracerebroventricular administration of histaminergic drugs on morphine state-dependent memory in the step-down passive avoidance test.
2005 May
Cross state-dependent retrieval between histamine and lithium.
2005 Sep 15
Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors.
2006 Apr
Histamine increases sickle erythrocyte adherence to endothelium.
2006 Feb
N-(4-Trifluoromethylphenyl)amide group of the synthetic histamine receptor agonist inhibits nicotinic acetylcholine receptor-mediated catecholamine secretion.
2006 Feb 28
Effects of intracerebroventricular administration of ultra low doses of histaminergic drugs on morphine state-dependent memory of passive avoidance in mice.
2006 Jan 6
STAT1 phosphorylation and cleavage is regulated by the histamine (H4) receptor in human atopic and non-atopic lymphocytes.
2006 Oct
Role of apolipoprotein E in anxiety.
2007
Role of histamine in ghrelin-induced gastroprotection against acute gastric lesions.
2007 Apr
Histamine downregulates monocyte CCL2 production through the histamine H4 receptor.
2007 Aug
Pre-synaptic histamine H3 receptors regulate glutamate, but not GABA release in rat thalamus.
2007 Feb
The human histamine H3 receptor couples to GIRK channels in Xenopus oocytes.
2007 Jul 19
[Reversing effect of histamine on neurotoxicity induced by beta-amyloid1-42].
2007 Mar
Histamine augments beta2-adrenoceptor-induced cyclic AMP accumulation in human prostate cancer cells DU-145 independently of known histamine receptors.
2007 Mar 15
Substance P is involved in the effect of histamine H3 receptor agonist, Sch 50971 on nasal allergic symptoms in mice.
2008 Aug
Human inflammatory dendritic epidermal cells express a functional histamine H4 receptor.
2008 Jul
Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells.
2008 Jun 6
Apomorphine-induced turning behavior in 6-hydroxydopamine lesioned rats is increased by histidine and decreased by histidine decarboxylase, histamine H1 and H2 receptor antagonists, and an H3 receptor agonist.
2008 Sep
Substance Class Chemical
Created
by admin
on Fri Dec 16 23:47:14 UTC 2022
Edited
by admin
on Fri Dec 16 23:47:14 UTC 2022
Record UNII
RKU631JF4H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CLOBENPROPIT
Common Name English
VUF-9153
Code English
CARBAMIMIDOTHIOIC ACID, N-((4-CHLOROPHENYL)METHYL)-, 3-(1H-IMIDAZOL-5-YL)PROPYL ESTER
Systematic Name English
Code System Code Type Description
CAS
145231-45-4
Created by admin on Fri Dec 16 23:47:14 UTC 2022 , Edited by admin on Fri Dec 16 23:47:14 UTC 2022
PRIMARY
EPA CompTox
DTXSID3043738
Created by admin on Fri Dec 16 23:47:14 UTC 2022 , Edited by admin on Fri Dec 16 23:47:14 UTC 2022
PRIMARY
WIKIPEDIA
Clobenpropit
Created by admin on Fri Dec 16 23:47:14 UTC 2022 , Edited by admin on Fri Dec 16 23:47:14 UTC 2022
PRIMARY
FDA UNII
RKU631JF4H
Created by admin on Fri Dec 16 23:47:14 UTC 2022 , Edited by admin on Fri Dec 16 23:47:14 UTC 2022
PRIMARY
PUBCHEM
2790
Created by admin on Fri Dec 16 23:47:14 UTC 2022 , Edited by admin on Fri Dec 16 23:47:14 UTC 2022
PRIMARY
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