| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
Pentiapine's primary mechanism of action is as a dopamine release inhibitor. It does not bind to synaptic dopamine receptor sites, distinguishing it from classical antipsychotics that act as postsynaptic receptor antagonists. It was initially developed to modulate central nervous system neurotransmission by antagonizing multiple neurotransmitter receptors, particularly dopamine D2 and serotonin 5-HT2A receptors. Through its dual dopaminergic and serotonergic actions, Pentiapine exhibits both antipsychotic and sedative effects. This mechanism of action is similar to other atypical antipsychotics like quetiapine, but its primary function as a dopamine release inhibitor sets it apart.
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| ln Vitro |
In vitro, Pentiapine functions as a novel inhibitor of dopamine release. It does not bind to synaptic dopamine receptor sites, indicating a unique mechanism of action compared to typical antipsychotics. It has been shown to modulate dopaminergic and serotonergic signaling, which are key pathways involved in the pathophysiology of schizophrenia and other psychiatric disorders. Quantitative in vitro activity data, such as IC50 values for dopamine release inhibition, is not detailed in the publicly available sources.
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| ln Vivo |
A brand-new dopamine release inhibitor is called pentiapine. The findings demonstrated that mice's locomotor activity was dose-dependently decreased by pentiapine. Moreover, morphine-induced hyperactivity was decreased by pentiapine in a dose-dependent manner. The group that received both saline and morphine had greater activity, according to Newman-Keuls post hoc comparisons. Furthermore, morphine plus 0.5, 1, and 2 mg/kg pentiapine groups exhibited increased activity (P<0.01) compared to morphine plus 4, 8, 16, 24, and 32 mg/kg pentiapine groups [1]. When administered at a dose of 30 mg/kg, pentiapine totally inhibits both the development of cocaine CPP and the conditioned place preference (CPP) to methylenedioxymethamphetamine (MDMA) [2].
In vivo, Pentiapine dose-dependently reduces motor activity in mice. It also dose-dependently reduces morphine-induced hyperactivity, suggesting its potential in modulating reward pathways. These in vivo effects are consistent with its mechanism as a dopamine release inhibitor and its sedative properties. It has been studied for potential use in treating schizophrenia, including hallucinations, delusions, disorganized thinking, and affective disturbances. The compound's effects on motor activity and its ability to attenuate morphine-induced hyperactivity make it a useful tool for studying dopaminergic function and antipsychotic activity in vivo. |
| Enzyme Assay |
For in vitro cell-free assays, the primary target of Pentiapine is dopamine release, which is not a cell-free enzyme or receptor binding event. Therefore, standard cell-free assays for receptor binding are not applicable as Pentiapine does not bind to synaptic dopamine receptor sites. Its activity can be studied in synaptosome preparations, where the inhibition of evoked dopamine release can be measured. In these assays, synaptosomes are loaded with a radioactive tracer like [3H]dopamine, and the amount of neurotransmitter released upon depolarization (e.g., with high potassium) is measured in the presence and absence of Pentiapine.
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| Cell Assay |
For in vitro cellular assays, the effect of Pentiapine on dopamine release can be studied using primary neuronal cultures or cell lines that express the machinery for dopamine synthesis and release. Cells are pre-loaded with a fluorescent dopamine analog or [3H]dopamine. After washing, cells are treated with Pentiapine and then stimulated to release dopamine (e.g., by depolarization with KCl). The amount of dopamine released into the medium is quantified using liquid scintillation counting (for radioactive label) or HPLC with electrochemical detection. The reduction in dopamine release in the presence of Pentiapine is measured, and the IC50 for inhibition is determined.
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| Animal Protocol |
For in vivo studies, the effects of Pentiapine are typically evaluated in rodent models of psychostimulant-induced hyperactivity or in models of schizophrenia. For example, mice are administered Pentiapine (e.g., via intraperitoneal injection) prior to receiving a dose of morphine or amphetamine. The locomotor activity of the animals is then measured using an automated activity chamber. The reduction in hyperactivity induced by the psychostimulant is a measure of the compound's antipsychotic-like activity. Its effect on motor activity can also be assessed independently. These behavioral assays are used to confirm its dopamine release inhibitory and sedative properties in vivo.
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| ADME/Pharmacokinetics |
Pentiapine (C18H20N4S) has a molecular weight of 324.44 g/mol. The CAS number is 81382-51-6. It is typically supplied as a powder. For in vitro studies, it is dissolved in DMSO to prepare stock solutions. For in vivo administration, it can be formulated in suitable vehicles, such as saline or a mixture of DMSO and PEG. Storage is recommended at -20°C, protected from light. Its purity is typically >98% for research use.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As an antipsychotic compound, potential side effects may include sedation, extrapyramidal symptoms, and metabolic effects, though its unique mechanism as a dopamine release inhibitor may confer a different side-effect profile compared to classical antipsychotics. Standard toxicological studies would be required for drug development.
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| References |
[1]. Manzanedo C, et al. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32.
[2]. Bilsky EJ, et al. CGS 10746B, a novel dopamine release inhibitor, blocks the establishment of cocaine and MDMA conditioned place preferences. Pharmacol Biochem Behav. 1998 Jan;59(1):215-20 |
| Additional Infomation |
Pentiapine is an aryl sulfide.
Pentiapine is a research-grade compound and is not approved for any therapeutic use. It serves primarily as a valuable pharmacological tool for studying dopamine release and antipsychotic activity. Its mechanism of action involves the inhibition of dopamine release without binding to postsynaptic dopamine receptors. This unique profile makes it a useful compound for investigating the role of dopamine in neuropsychiatric disorders and for developing novel therapeutic strategies. No clinical trials have been reported. |
| Molecular Formula |
C15H17N5S
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| Molecular Weight |
299.39398
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| Exact Mass |
299.12
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| CAS # |
81382-51-6
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| PubChem CID |
54742
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.442
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
407
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C2SC3C(N=C(N2C=C1)N1CCN(C)CC1)=CC=CC=3
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| InChi Key |
FACMWMBWGSPRKO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17N5S/c1-18-8-10-19(11-9-18)14-17-12-4-2-3-5-13(12)21-15-16-6-7-20(14)15/h2-7H,8-11H2,1H3
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| Chemical Name |
5-(4-methylpiperazin-1-yl)imidazo[2,1-b][1,3,5]benzothiadiazepine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3401 mL | 16.7006 mL | 33.4012 mL | |
| 5 mM | 0.6680 mL | 3.3401 mL | 6.6802 mL | |
| 10 mM | 0.3340 mL | 1.6701 mL | 3.3401 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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