Thioperamide maleate
Based on 3 publication(s) in Google Scholar
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM.
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- Reinheit : 98.26%
- CAS. Nr.: 148440-81-7
- Formel: C15H24N4S.xC4H4O4
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Thioperamide maleate
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
H3 Receptor |
In Vitro
Thioperamide inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM[1].
Thioperamide (0.01-100 μM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner[2].
Thioperamide displays similar potencies at human H4 and H3 receptors (Ki=43 and 60 nM, respectively)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:NE-4C stem cells
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Concentration:0.01, 0.1, 1, 10, 100 μM
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Incubation Time:24 hours
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Result:The viability of NE-4C stem cells increased significantly to 150.83±6.91% when (1 μM) was administrated, and increased to 145.11±14.52% and 132.02%±25.65% when 10 μM and 100 μM were administrated respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naive female C57BL/6J mice[4]
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Dosage:5, 10 or 20 mg/kg
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Administration:Injections (i.p.)
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Result:Facilitated reconsolidation of a contextually-conditioned fear memory.
Chemical Information
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CAS. Nr. 148440-81-7
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Appearance Solid
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Formel C15H24N4S.xC4H4O4
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Color White to off-white
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SMILES
S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3.O=C(O)/C=C\C(O)=O.[x]
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Synonyms
MR-12842 maleate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Eur J Pharmacol
The role of heterodimers formed by histamine H3 receptors and dopamine D1 receptors on the methamphetamine-induced conditioned place preference. [Abstract]2024 Oct 15:981:176866. PMID: 39089461
Lösungsmittel & Löslichkeit
In Vitro:
H2O : 100 mg/mL (Need ultrasonic)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23. [Content Brief]
[2]. Na Wang, et al. Histamine H3 Receptor Antagonist Enhances Neurogenesis and Improves Chronic Cerebral Hypoperfusion-Induced Cognitive Impairments. Front Pharmacol. 2020 Jan 21;10:1583. [Content Brief]
[3]. Y Charlier, et al. Differential Effects of Histamine H(3) Receptor Inverse Agonist Thioperamide, Given Alone or in Combination With the N-methyl-d-aspartate Receptor Antagonist Dizocilpine, on Reconsolidation and Consolidation of a Contextual Fear Memory in Mice. Neuroscience. 2011 Oct 13;193:132-42. [Content Brief]
[4]. Gbahou F, et al. Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br J Pharmacol. 2006;147(7):744-754. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Thioperamide maleate Related Classifications
HY-12206A Related Classifications
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