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
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)
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL264 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20833043 |
1.0 nM [IC50] |
PubMed
Title | Date | PubMed |
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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 |
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Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. | 2000 Dec |
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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 |
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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 |
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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
Edited
Fri Dec 16 23:47:14 UTC 2022
by
admin
on
Fri Dec 16 23:47:14 UTC 2022
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Record UNII |
RKU631JF4H
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Record Status |
Validated (UNII)
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Record Version |
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-
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Code | English | ||
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Systematic Name | English |
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145231-45-4
Created by
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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
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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
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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
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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
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |