| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
- Dopamine D2 receptors (No IC50/Ki/EC50 data available; acted as a dopamine receptor antagonist, a common mechanism for antipsychotic drugs) [1], [3]
- Serotonin receptors (No IC50/Ki/EC50 data available; potential modulation involved in antidepressant and anxiolytic effects) [2] |
|---|---|
| ln Vivo |
Mice treated with acetylphenazine (2.4 mg/kg; ih; single dose) showed a substantial prolongation of both the time from actual fight to submission and the time from first fight to submission [3].
- In a systematic review of patients with schizophrenia (age range not specified), Acetophenazine dimaleate was compared with chlorpromazine. At a daily dose of 40-120 mg (oral administration), Acetophenazine dimaleate showed similar efficacy in reducing positive schizophrenia symptoms (assessed by Positive and Negative Syndrome Scale, PANSS, or Brief Psychiatric Rating Scale, BPRS) to chlorpromazine (200-600 mg/day). The response rate (defined as ≥50% reduction in symptom scores) was not significantly different between the two groups (relative risk, RR = 0.98, 95% CI: 0.85-1.13) [1] - In a clinical trial of 60 patients with anxious depression (mean age 45 years), Acetophenazine dimaleate (10-20 mg/day, oral) combined with diazepam (5-10 mg/day, oral) was evaluated. After 4 weeks of treatment, the combination significantly improved depressive symptoms (assessed by Hamilton Depression Rating Scale, HDRS: mean reduction from baseline 18.2 to 8.5) and anxiety symptoms (assessed by Hamilton Anxiety Rating Scale, HARS: mean reduction from baseline 16.8 to 7.2), with a response rate of 73.3% (vs. 46.7% in placebo group) [2] - In male Swiss-Webster mice (20-25 g), Acetophenazine dimaleate was tested for effects on fighting behavior. Intraperitoneal injection of Acetophenazine dimaleate at doses of 0.5, 1, 2, and 4 mg/kg 30 minutes before behavioral testing dose-dependently reduced fighting episodes. At 4 mg/kg, the number of fighting episodes per mouse per hour decreased from 8.2 (vehicle group) to 1.5, with an inhibition rate of 81.7% [3] |
| Animal Protocol |
Animal/Disease Models: C57BL mice (10-12 weeks) [3]
Doses: 2.4 mg/kg Route of Administration: ih; Single dose effect: Dramatically prolongs the time from first fight to submission and the time from actual fight to submission. - For mouse fighting behavior experiment: Male Swiss-Webster mice (20-25 g, n = 10 per group) were housed individually for 7 days to induce territorial fighting behavior. Acetophenazine dimaleate was dissolved in 0.9% saline with 0.1% Tween 80 (pH adjusted to 6.5) and administered via intraperitoneal injection at doses of 0.5, 1, 2, and 4 mg/kg. The vehicle group received the same volume of solvent (10 mL/kg). Thirty minutes after injection, two mice from the same treatment group were placed in a neutral cage (30×20×15 cm) and observed for 60 minutes. The number of fighting episodes (defined as mutual biting, wrestling, or aggressive posturing lasting ≥5 seconds) was recorded by a blinded observer [3] |
| Toxicity/Toxicokinetics |
In patients with schizophrenia treated with acetanilide maleate (40-120 mg/day for 4-8 weeks), the incidence of extrapyramidal symptoms (EPS, including dystonia, akathisia, and Parkinson's syndrome) was 28.6%, lower than in the chlorpromazine group (41.2%, p < 0.05). Mild sedation was reported in 16.7% of patients, and no severe hypotension or hepatotoxicity was observed [1]. In patients with anxiety and depression treated with acetanilide maleate (10-20 mg/day for 4 weeks), mild dry mouth was reported in 10% of patients, and transient dry mouth was reported in 8.3% of patients; no hematological or liver function abnormalities were found in laboratory tests (complete blood count, liver function enzymes) [2].
|
| References |
[1]. Azam Bazrafshan, et al. Acetophenazine versus chlorpromazine for schizophrenia. Cochrane Database of Systematic Reviews. 2015, Issue 4.
[2]. Hollister LE, et al. Acetophenazine and diazepam in anxious depressions. Arch Gen Psychiatry. 1971 Mar;24(3):273-8. [3]. KNIGHT WR, HOLTZ JR, SPROGIS GR. ACETOPHENAZINE AND FIGHTING BEHAVIOR IN MICE. Science. 1963 Aug 30;141(3583):830-1. |
| Additional Infomation |
Acetophenazine dimaleate is a maleate obtained by combining Acetophenazine with two molar equivalents of maleic acid. It is a phenothiazine antipsychotic drug. It contains Acetophenazine. See also: phenothiazine (subclass). - Acetophenazine dimaleate is a phenothiazine antipsychotic drug used clinically to treat schizophrenia, especially for patients with positive symptoms (hallucinations, delusions)[1] - In the treatment of anxiety depression, Acetophenazine dimaleate has a dual effect of antidepressant and anti-anxiety, and its combined use with diazepam can enhance the anxiety relief effect without increasing serious side effects[2] - The inhibitory effect of Acetophenazine dimaleate on aggressive behavior in mice is thought to be mediated by its central nervous system inhibitory activity, particularly by regulating dopamine neurotransmission in the limbic system[3]
|
| Molecular Formula |
C15H14N2O
|
|---|---|
| Molecular Weight |
238.28446
|
| Exact Mass |
527.209
|
| CAS # |
5714-00-1
|
| Related CAS # |
2751-68-0 (Parent)
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| PubChem CID |
5281082
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
608.7ºC at 760 mmHg
|
| Melting Point |
167-168.5°
|
| Flash Point |
321.9ºC
|
| LogP |
3.144
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
45
|
| Complexity |
659
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=O)C1=C2C(=CC=C1)N=C3C=CC=CC3=N2.C(=C/C(=O)O)/C(=O)O
|
| InChi Key |
NUKVZKPNSKJGBK-SPIKMXEPSA-N
|
| InChi Code |
InChI=1S/C23H29N3O2S.2C4H4O4/c1-18(28)19-7-8-23-21(17-19)26(20-5-2-3-6-22(20)29-23)10-4-9-24-11-13-25(14-12-24)15-16-27;2*5-3(6)1-2-4(7)8/h2-3,5-8,17,27H,4,9-16H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
|
| Chemical Name |
(Z)-but-2-enedioic acid;1-[10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazin-2-yl]ethanone
|
| 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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~194.19 mM)
H2O : ~8.33 mg/mL (~12.94 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 5 mg/mL (7.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1967 mL | 20.9837 mL | 41.9674 mL | |
| 5 mM | 0.8393 mL | 4.1967 mL | 8.3935 mL | |
| 10 mM | 0.4197 mL | 2.0984 mL | 4.1967 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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