Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C6H15N3S |
| Molecular Weight | 161.268 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCCSC(N)=N
InChI
InChIKey=OLHQOJYVQUNWPL-UHFFFAOYSA-N
InChI=1S/C6H15N3S/c1-9(2)4-3-5-10-6(7)8/h3-5H2,1-2H3,(H3,7,8)
| Molecular Formula | C6H15N3S |
| Molecular Weight | 161.268 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25524412 | https://www.ncbi.nlm.nih.gov/pubmed/21211106
Curator's Comment: Dimaprit is CNS active in animals. No human data available.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Involvement of histaminergic receptor mechanisms in the stimulation of NT-3 synthesis in astrocytes. | 2011-06 |
|
| The effect of intracerebroventricular injection of histamine in visceral nociception induced by acetic acid in rats. | 2010-10 |
|
| Control of the flow properties of DNA by topoisomerase II and its targeting inhibitor. | 2010-09-22 |
|
| Persistent oxygen-glucose deprivation induces astrocytic death through two different pathways and calpain-mediated proteolysis of cytoskeletal proteins during astrocytic oncosis. | 2010-07-26 |
|
| Histamine inhibits adhesion molecule expression in human monocytes, induced by advanced glycation end products, during the mixed lymphocyte reaction. | 2010-07 |
|
| Activation of adenosine low-affinity A3 receptors inhibits the enteric short interplexus neural circuit triggered by histamine. | 2009-12 |
|
| Regulation of human umbilical artery contractility by different serotonin and histamine receptors. | 2009-12 |
|
| Histamine inhibits advanced glycation end products-induced adhesion molecule expression on human monocytes. | 2009-09 |
|
| Differential role of beta-catenin in VEGF and histamine-induced MMP-2 production in microvascular endothelial cells. | 2009-05-15 |
|
| Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430. | 2009-05 |
|
| Histamine responses of large neostriatal interneurons in histamine H1 and H2 receptor knock-out mice. | 2009-03-16 |
|
| Cytokine responses of intraepithelial lymphocytes are regulated by histamine H(2) receptor. | 2009 |
|
| G-protein coupled receptor signaling architecture of mammalian immune cells. | 2009 |
|
| Histamine excites rat lateral vestibular nuclear neurons through activation of post-synaptic H2 receptors. | 2008-12-19 |
|
| Agonist-induced internalization of histamine H2 receptor and activation of extracellular signal-regulated kinases are dynamin-dependent. | 2008-10 |
|
| Histamine-induced itch and its relationship with pain. | 2008-07-31 |
|
| Validation of a conscious rat model for the discovery of novel agents that inhibit gastric acid secretion. | 2008-07-28 |
|
| Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells. | 2008-06-06 |
|
| The ATPase cycle of the mitochondrial Hsp90 analog Trap1. | 2008-04-25 |
|
| Suppression of ischaemia-induced cytokine release by dimaprit and amelioration of liver injury in rats. | 2008-04 |
|
| Histamine metabolism influences blood vessel branching in zebrafish reg6 mutants. | 2008-03-25 |
|
| The anti-secretory and anti-ulcer activities of esomeprazole in comparison with omeprazole in the stomach of rats and rabbits. | 2008-02 |
|
| Olfactory interference during inhibitory backward pairing in honey bees. | 2008 |
|
| Histamine excites neurones in the human submucous plexus through activation of H1, H2, H3 and H4 receptors. | 2007-09-01 |
|
| Histamine ameliorates anti-glomerular basement membrane antibody-induced glomerulonephritis in rats. | 2007-09 |
|
| Blockade of brain histamine metabolism alters methamphetamine-induced expression pattern of stereotypy in mice via histamine H1 receptors. | 2007-07-13 |
|
| Histamine H4 receptor agonists have more activities than H4 agonism in antigen-specific human T-cell responses. | 2007-06 |
|
| Study on the antinociceptive action of Tyr-K-MIF-1, a peptide from the MIF family. | 2007-04 |
|
| Modification of formalin-induced nociception by different histamine receptor agonists and antagonists. | 2007-01-15 |
|
| Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats. | 2006-08-21 |
|
| Histamine enhances inhibitory avoidance memory consolidation through a H2 receptor-dependent mechanism. | 2006-07 |
|
| Histamine receptors in human detrusor smooth muscle cells: physiological properties and immunohistochemical representation of subtypes. | 2006-06 |
|
| Cultured smooth muscle cells of the human vesical sphincter are more sensitive to histamine than are detrusor smooth muscle cells. | 2006-05 |
|
| Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. | 2006-04 |
|
| The protective effect of H2-receptor activation against the duration of myocardial hypoxia/reoxygenation-induced ventricular fibrillation in sensitized guinea-pig hearts. | 2005-12 |
|
| Curcuma longa extract protects against gastric ulcers by blocking H2 histamine receptors. | 2005-12 |
|
| Excitatory effect of histamine on neuronal activity of rat globus pallidus by activation of H2 receptors in vitro. | 2005-11 |
|
| Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. | 2005-09 |
|
| Histamine helps development of eczematous lesions in experimental contact dermatitis in mice. | 2005-08 |
|
| Histamine receptors that influence blockage of the normal human nasal airway. | 2005-03 |
|
| Effects of activation of central nervous histamine receptors in cardiovascular regulation; studies in H(1) and H(2) receptor gene knockout mice. | 2005-02 |
|
| Histamine contributes to ischemia-related activation of cardiac spinal afferents: role of H1 receptors and PKC. | 2005-02 |
|
| Replacement of amino acid sequence features of a- and c-subunits of ATP synthases of Alkaliphilic Bacillus with the Bacillus consensus sequence results in defective oxidative phosphorylation and non-fermentative growth at pH 10.5. | 2004-06-18 |
|
| The effects of histamine on rat and monkey retinal ganglion cells. | 2004-06-14 |
|
| Involvement of histamine H4 and H1 receptors in scratching induced by histamine receptor agonists in Balb C mice. | 2004-05 |
|
| Involvement of H2-receptors in the mechanism of analgesic action of Tyr-MIF-1. | 2003-12 |
|
| Regulation of interleukin-6, and macrophage colony-stimulating factor mRNA levels by histamine in stromal cell line (MC3T3-G2/PA6). | 1998-05 |
|
| Histamine modulates the expression of c-fos through cyclic AMP production via the H2 receptor in the human promonocytic cell line U937. | 1997-06 |
|
| Efficacy of a selective histamine H2 receptor agonist, dimaprit, in experimental models of endotoxin shock and hepatitis in mice. | 1997-03-12 |
|
| Effect of adenosine and histamine receptor stimulation on canine histamine release to pentagastrin. | 1997 |
Patents
Sample Use Guides
In vitro, dimaprit dose dependently inhibited the production of TNF-alpha in mouse peritoneal macrophages and human peripheral blood monocytes stimulated with lipopolysaccharide with IC50 values of 1 uM.
Dimaprit, added to tumour cell cultures (100 uM), inhibited the incorporation of 3H-thymidine while embryonic cell cultures were unaffected.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 19:56:17 GMT 2025
by
admin
on
Mon Mar 31 19:56:17 GMT 2025
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| Record UNII |
ZZQ699148P
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| Record Status |
Validated (UNII)
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| Record Version |
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Common Name | English | ||
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Preferred Name | English |
| Code System | Code | Type | Description | ||
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DIMAPRIT
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65119-89-3
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DTXSID0037154
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ZZQ699148P
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3077
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admin on Mon Mar 31 19:56:18 GMT 2025 , Edited by admin on Mon Mar 31 19:56:18 GMT 2025
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