| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Acetophenazine acts primarily as a dopamine D2 receptor antagonist. It also exhibits activity at serotonin receptors, particularly 5-HT6 receptors. As a phenothiazine antipsychotic, its mechanism of action involves blocking dopamine receptors in the central nervous system, thereby modulating dopaminergic neurotransmission involved in the regulation of mood, behavior, and cognition. The compound's anxiolytic properties suggest additional effects on other neurotransmitter systems.
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| ln Vitro |
Acetophenazine demonstrates antipsychotic and anxiolytic activity in various in vitro and in vivo models. As a dopamine D2 receptor antagonist, it inhibits dopamine-mediated signaling in the central nervous system. The compound's activity at serotonin receptors, particularly 5-HT6, may contribute to its overall pharmacological profile. However, detailed in vitro activity data including IC50 values for specific receptor targets are limited. Further studies are needed to fully characterize its receptor binding profile and functional activity.
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| 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].
Acetophenazine is used as an antipsychotic and anxiolytic agent in clinical settings. It has been studied for its efficacy in treating depression and anxiety disorders. The compound's moderate potency and side effect profile have been characterized in clinical studies. However, detailed in vivo activity data including specific dosing regimens and clinical outcomes are limited in the publicly available literature. |
| Enzyme Assay |
Receptor binding assays using radiolabeled ligands to evaluate Acetophenazine's affinity for dopamine D2 receptors, serotonin receptors (5-HT6, 5-HT2A), and other CNS targets. Competition binding experiments are performed using membrane preparations from cells expressing recombinant receptors or from brain tissue, incubated with increasing concentrations of Acetophenazine and a fixed concentration of a selective radioligand. Nonspecific binding is determined in the presence of an excess of unlabeled competitor. Bound radioactivity is measured by scintillation counting, and IC50 values are calculated from competition curves, which are then converted to Ki values using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cell-based assays using neuronal cell lines or cells expressing recombinant dopamine or serotonin receptors to evaluate the effects of Acetophenazine on receptor signaling. Cells are treated with Acetophenazine at various concentrations, and receptor activation is assessed by measuring downstream signaling pathways (e.g., cAMP levels, calcium mobilization, or reporter gene activity). Cell viability is assessed using MTT or CellTiter-Glo assays. The compound's effects on neurotransmitter uptake or release may also be evaluated.
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| 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. In vivo studies in rodent models of psychiatric disorders to evaluate the antipsychotic and anxiolytic effects of Acetophenazine. Acetophenazine is administered via various routes (i.p., p.o., or s.c.) at doses ranging from 0.1 to 10 mg/kg. Behavioral assays such as the open field test, elevated plus maze, forced swim test, and prepulse inhibition of startle are used to assess anxiety-like and depressive-like behaviors. Locomotor activity is monitored to assess sedative effects. Receptor occupancy studies using PET imaging with selective radiotracers can be performed to confirm target engagement in the brain. Pharmacokinetic parameters including brain penetration are determined following administration. |
| References | |
| Additional Infomation |
Acetylphenazine belongs to the phenothiazine class of compounds, with the structure 10H-phenothiazine, where the nitrogen atom is substituted with a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group and the 2-position is substituted with an acetyl group. It is a phenothiazine antipsychotic drug. Acetylphenazine belongs to the phenothiazine, N-alkylpiperazine, and N-(2-hydroxyethyl)piperazine classes, and its function is related to that of 10H-phenothiazine compounds. Acetylphenazine is a moderately potent antipsychotic drug used to treat confusion and psychotic symptoms, and can also be used as an adjunct treatment for illusions (such as hallucinations or delusions). It primarily acts on dopamine D2 receptors. Drug Indications Used to treat confusion and psychotic symptoms. Also used to help treat delusions (such as hallucinations or delusions). Mechanism of Action Acetylbenzamine blocks postsynaptic mesolimbic dopamine D1 and D2 receptors in the brain; it inhibits the release of hypothalamic and pituitary hormones and is believed to inhibit the reticular activating system, thereby affecting basal metabolism, body temperature, arousal, vasomotor activity, and vomiting. Pharmacodynamics Acetylbenzamine is a phenothiazine antipsychotic drug used to treat schizophrenia and other psychotic disorders.
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| Molecular Formula |
C23H29N3O2S
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|---|---|
| Molecular Weight |
411.56026
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| Exact Mass |
411.198
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| CAS # |
2751-68-0
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| Related CAS # |
Acetophenazine-d4 dimaleate
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| PubChem CID |
17676
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| Appearance |
Light yellow to yellow solid
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| Density |
1.203g/cm3
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| Boiling Point |
608.7ºC at 760mmHg
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| Melting Point |
167-168.5
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| Flash Point |
321.9ºC
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| Vapour Pressure |
7.83E-16mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
3.432
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
540
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCCN1CCN(CCCN2C3=C(C=CC(C(=O)C)=C3)SC3C2=CC=CC=3)CC1
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| InChi Key |
WNTYBHLDCKXEOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H29N3O2S/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/h2-3,5-8,17,27H,4,9-16H2,1H3
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| Chemical Name |
1-[10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazin-2-yl]ethanone
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| Synonyms |
AcetophenazineTindal Acephenazinum
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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: ~100 mg/mL (~243.0 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4298 mL | 12.1489 mL | 24.2978 mL | |
| 5 mM | 0.4860 mL | 2.4298 mL | 4.8596 mL | |
| 10 mM | 0.2430 mL | 1.2149 mL | 2.4298 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05846438 | Recruiting | Other: Showering 48 hours after surgery |
Infections Quality of Life |
University of Missouri-Columbia | March 15, 2023 | Not Applicable |
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