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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| Targets |
H3 Receptor
Histamine H3 receptor (primary target). Thioperamide maleate is a potent and selective H3 receptor antagonist. It also displays similar potencies at human H4 receptors (Ki = 43 nM). |
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| ln Vitro |
With Kis of 2.1 nM and 2.0 nM, respectively, thioperamide inhibits [3H]-(R)α-MeHA binding in the lung of guinea pigs and the brain of rats. With a mean apparent Ki of 4 nM, thioperamide competitively inhibits H3-autoreceptors that control the release of [3H]histones[1]. In a concentration-dependent manner, thioperamide (0.01-100 μM; 24 hours) increases the vitality of NE-4C stem cells[2]. At human H4 and H3 receptors, thioperamide has comparable potencies (Ki=43 and 60 nM, respectively)[3].
Thioperamide is a highly potent H3 receptor antagonist, inhibiting [3H]-[R]α-MeHA binding in rat brain and guinea-pig lung with Ki values of 2.1 nM and 2.0 nM, respectively. It competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM. In a cell viability assay using NE-4C stem cells, Thioperamide (0.01-100 μM; 24 hours) promoted cell viability in a concentration-dependent manner, with a significant increase to 150.83±6.91% at 1 μM. The compound also displays similar potencies at human H4 and H3 receptors (Ki = 43 and 60 nM, respectively). |
| ln Vivo |
In C57BL/6J mice, thioperamide (5–20 mg/kg; ip) can help reconsolidate a contextually-conditioned fear memory[4].
In vivo, Thioperamide (5-20 mg/kg; intraperitoneal injection) facilitates the reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice. It affects the central histaminergic system and decreases the duration of seizures and convulsions in mice. It also improves learning deficits induced by other drugs such as scopolamine. Additionally, Thioperamide enhances neurogenesis and improves chronic cerebral hypoperfusion-induced cognitive impairments. These findings highlight its potential as a cognitive enhancer and neuroprotective agent. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Thioperamide are performed to evaluate its affinity for the H3 receptor. Radioligand binding studies using membrane preparations from cells or tissues expressing the H3 receptor, such as rat brain or guinea-pig lung, are conducted. The compound's ability to displace a specific radiolabeled H3 ligand, such as [3H]-[R]α-MeHA, is measured to calculate its Ki values. Functional assays are also used to assess its antagonist activity by measuring its ability to block H3 receptor-mediated inhibition of [3H]histamine release.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: NE-4C stem cells Tested Concentrations: 0.01, 0.1, 1, 10, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: The viability of NE-4C stem cells increased Dramatically to 150.83±6.91% when (1 μM) was administered, and increased to 145.11±14.52% and 132.02%±25.65% when 10 μM and 100 μM were administered respectively. In vitro cell-based assays are conducted to evaluate the effects of Thioperamide on cell viability and function. For example, NE-4C stem cells are treated with Thioperamide at various concentrations (0.01-100 μM) for 24 hours, and cell viability is assessed using standard assays such as MTT or CCK-8. The compound has been shown to promote cell viability in a concentration-dependent manner. These assays help to characterize the cellular effects of H3 receptor antagonism and its potential role in neurogenesis. |
| Animal Protocol |
Animal/Disease Models: Naive female C57BL/6J mice[4]
Doses: 5, 10 or 20 mg/kg Route of Administration: Injections (ip) Experimental Results: Facilitated reconsolidation of a contextually-conditioned fear memory. In vivo animal studies are conducted in rodent models to evaluate the pharmacological effects of Thioperamide. The compound is typically administered via intraperitoneal injection at doses ranging from 5 to 20 mg/kg. Its effects on cognitive function are assessed using behavioral tests such as fear conditioning, novel object recognition, and Morris water maze. Its anticonvulsant activity is evaluated in seizure models. Additionally, its effects on neurogenesis and cerebral blood flow are investigated in models of chronic cerebral hypoperfusion. |
| ADME/Pharmacokinetics |
Thioperamide is an orally active compound that crosses the blood-brain barrier. Detailed pharmacokinetic parameters such as half-life, bioavailability, and volume of distribution are not extensively documented in publicly available literature. As a lipophilic small molecule, it is expected to be well-absorbed from the gastrointestinal tract and distributed throughout the body, including the central nervous system. It is likely metabolized in the liver and excreted via the kidneys. Its ability to cross the blood-brain barrier is a key feature for its use in central nervous system research.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for Thioperamide maleate. As a research compound, its toxicity profile is expected to be related to its mechanism of action as a histamine H3 receptor antagonist. H3 receptor antagonists are generally well-tolerated, but may cause side effects related to increased histaminergic and cholinergic neurotransmission, such as insomnia, anxiety, or gastrointestinal disturbances. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
See other relationships...
Thioperamide maleate (MR-12842 maleate) is a potent, selective, and orally active H3 receptor antagonist that crosses the blood-brain barrier. It is a widely used pharmacological tool for studying the central histaminergic system. Thioperamide inhibits [3H]histamine release (Ki = 4.3 nM) and synthesis (Ki = 31 nM). It has been shown to facilitate fear memory reconsolidation, decrease seizure duration, and improve learning deficits. The compound is not approved for human therapeutic use and is strictly for research purposes. |
| Molecular Weight |
408.5150
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| Exact Mass |
408.183
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| CAS # |
148440-81-7
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| PubChem CID |
11211984
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| Appearance |
White to off-white solid powder
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| LogP |
2.836
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(CC1)NC(=S)N2CCC(CC2)C3=CN=CN3.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
WUYMIKDBRCCYGE-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C15H24N4S.C4H4O4/c20-15(18-13-4-2-1-3-5-13)19-8-6-12(7-9-19)14-10-16-11-17-14;5-3(6)1-2-4(7)8/h10-13H,1-9H2,(H,16,17)(H,18,20);1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4479 mL | 12.2393 mL | 24.4786 mL | |
| 5 mM | 0.4896 mL | 2.4479 mL | 4.8957 mL | |
| 10 mM | 0.2448 mL | 1.2239 mL | 2.4479 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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