| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vivo |
In the striatum of rats, thiopronazine (5 mg/kg; intraperitoneal injection; single dosage) enhances dopamine buildup [1].
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| Animal Protocol |
Animal/Disease Models: Male Charles River rat (200-250 g) [1].
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; single. Experimental Results: Significant reduction in dopamine levels (26%) and acceleration of dopamine synthesis and utilization in the striatum (250% enhancement in dopamine specific activity). |
| References |
[1]. Cheramy A, et al. Increased release of dopane from striatal dopaminergic terminals in the rat after treatment with a neuroleptic: thioproperazine. Eur J Pharmacol. 1970 May;10(2):206-14.
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| Additional Infomation |
Thiorprozin is a phenothiazine derivative with a dimethylaminosulfonyl substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl substituent at the N-10 position. It is a phenothiazine antipsychotic. It belongs to the phenothiazine, N-alkylpiperazine, N-methylpiperazine, and sulfonamide classes. Thiorprozin is a potent antipsychotic and neuroleptic. It exhibits significant rigidity and antiapomotor activity, along with relatively weak sedative, hypothermic, and antispasmodic effects. It has little to no antiserotonin or antihypertensive activity, and no antihistamine activity. It is used to treat various types of acute and chronic schizophrenia, including cases unresponsive to commonly used antipsychotics; mania.
Indications For the treatment of various types of acute and chronic schizophrenia, including cases unresponsive to commonly used antipsychotics; mania. Mechanism of Action Thioprozin acts as an antagonist (blocker) on different postsynaptic receptors—dopaminergic receptors (D1, D2, D3, and D4 subtypes—with different antipsychotic properties for productive and nonproductive symptoms), serotonergic receptors (5-HT1 and 5-HT2, with anti-anxiety, antidepressant, and anti-aggressive properties, and can reduce extrapyramidal side effects, but can also cause weight gain, hypotension, sedation, and ejaculatory dysfunction), histaminergic receptors (H1 receptors, with sedative, antiemetic, dizziness, hypotension, and weight gain effects), α1/α2 receptors, and α2 receptors. Receptors (which have anti-sympathetic properties, can lower blood pressure, cause reflex tachycardia and dizziness, sedation, excessive salivation and urinary incontinence, and sexual dysfunction, but may also alleviate pseudo-Parkinson's disease (controversial), and finally act on muscarinic (cholinergic) M1/M2 receptors (causing anticholinergic symptoms such as dry mouth, blurred vision, constipation, difficulty/inability to urinate, sinus tachycardia, ECG changes and memory loss, but anticholinergic effects may reduce extrapyramidal side effects). |
| Molecular Formula |
C22H30N4O2S2
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|---|---|
| Molecular Weight |
446.628
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| Exact Mass |
446.181
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| CAS # |
316-81-4
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| Related CAS # |
2347-80-0 (mesylate);316-81-4;
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| PubChem CID |
9429
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.237g/cm3
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| Boiling Point |
612.2ºC at 760mmHg
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| Melting Point |
140ºC
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| Flash Point |
324ºC
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| Index of Refraction |
1.615
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| LogP |
4.198
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
661
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C(C=C1N2CCCN3CCN(C)CC3)=CC=C1SC4=C2C=CC=C4)(N(C)C)=O
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| InChi Key |
VZYCZNZBPPHOFY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H30N4O2S2/c1-23(2)30(27,28)18-9-10-22-20(17-18)26(19-7-4-5-8-21(19)29-22)12-6-11-25-15-13-24(3)14-16-25/h4-5,7-10,17H,6,11-16H2,1-3H3
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| Chemical Name |
N,N-dimethyl-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine-2-sulfonamide
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| Synonyms |
Majeptyl; Cephalmin; Thioproperazine
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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 Vitro) |
DMSO : ~12.5 mg/mL (~27.99 mM ()
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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 | 2.2390 mL | 11.1949 mL | 22.3899 mL | |
| 5 mM | 0.4478 mL | 2.2390 mL | 4.4780 mL | |
| 10 mM | 0.2239 mL | 1.1195 mL | 2.2390 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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