| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary target of Propionylpromazine is the dopamine D2 receptor (DRD2), which it blocks as an antagonist. It also has antagonist activity at other neurotransmitter receptors, including histamine H1 receptors (contributing to sedation), adrenergic alpha1 receptors, and other dopamine receptor subtypes like D1 and D4, contributing to its overall neuroleptic profile.
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| ln Vitro |
In vitro, Propionylpromazine acts as an antagonist at the dopamine D2 receptor. It also has other identified activities, such as inhibiting recombinant T. cruzi trypanothione reductase (IC50 = 357 uM) and being active against T. brucei trypomastigotes (ED50 = 10.1 uM). However, its primary and most well-characterized activity is D2 receptor antagonism.
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| ln Vivo |
In vivo, Propionylpromazine is used as a sedative and tranquilizer in horses, camels, and other large animals. It demonstrates a distinct kinetic profile in camels with a 10-minute onset of action and a 2.1-hour duration, differing from other phenothiazines like acepromazine. It is also used to prevent stress and facilitate handling of animals.
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| Enzyme Assay |
The standard non-cellular protocol to determine D2 receptor binding affinity is a radioligand competition assay. Brain membranes (striatum) or membranes from cells expressing the recombinant human D2 receptor are incubated with [3H]spiperone (a D2 antagonist) and varying concentrations of Propionylpromazine. After incubation, bound vs. free ligand is separated by filtration, and IC50 is calculated.
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| Cell Assay |
Cell-based assays to measure functional antagonism of D2 receptors typically involve measuring cAMP accumulation. Cells expressing the D2 receptor are pre-treated with forskolin to stimulate cAMP production. Then, they are treated with a D2 agonist (like quinpirole) to inhibit cAMP, with or without Propionylpromazine. cAMP levels are quantified by HTRF. Propionylpromazine reverses the agonist-induced inhibition.
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| Animal Protocol |
Propionylpromazine is administered intramuscularly to horses for sedation. Blood samples are collected at various time points after administration. Plasma concentrations of propionylpromazine and its metabolites (2-(1-hydroxypropyl)promazine, etc.) are determined using gas chromatography or LC-MS to study its absorption, metabolism, and pharmacokinetic profile in the target species.
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| ADME/Pharmacokinetics |
Propionylpromazine has a protein binding of 81%, which may impact its bioavailability and distribution. In camels, it has a 10-minute onset and 2.1-hour duration of action. In horses, it is administered intramuscularly and is metabolized to several hydroxylated metabolites. It is not used in humans due to its side effect profile.
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| Toxicity/Toxicokinetics |
As a phenothiazine, Propionylpromazine can cause side effects related to its pharmacology, including extrapyramidal symptoms (tremors, rigidity), hypotension (due to alpha1-adrenergic blockade), and sedation (H1 blockade). In veterinary settings, it is used at doses that balance its sedative effects against these potential adverse events.
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| References |
[1]. A pharmacological network for lifespan extension in Caenorhabditis elegans. Aging Cell. 2014 Apr;13(2):206-15.
[2]. Metabolism and pharmacokinetic studies of propionylpromazine in horses. J Chromatogr. 1989 Apr 14;489(2):313-21. |
| Additional Infomation |
Propionylpromazine is the parent cpd
Propionylpromazine is distinct from many other phenothiazines (like chlorpromazine) in that its primary clinical use is almost exclusively in veterinary medicine rather than as a human antipsychotic. It is a classic example of a dopamine antagonist, and its use in animal models has contributed significantly to the pharmacological understanding of the D2 receptor's role in behavior and neurochemistry. |
| Molecular Formula |
C20H24N2OS
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|---|---|
| Molecular Weight |
340.48
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| Exact Mass |
340.161
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| CAS # |
3568-24-9
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| Related CAS # |
Propionylpromazine hydrochloride;7681-67-6
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| PubChem CID |
24352
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| Appearance |
Light green to green solid powder
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| Density |
1.138 g/cm3
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| Boiling Point |
507.4ºC at 760 mmHg
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| Flash Point |
260.7ºC
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| Index of Refraction |
1.601
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| LogP |
4.898
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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 |
6
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| Heavy Atom Count |
24
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCCN1C2=C(C=CC(C(=O)CC)=C2)SC2C1=CC=CC=2
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| InChi Key |
ZQTVCQIJTREKSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24N2OS/c1-4-18(23)15-10-11-20-17(14-15)22(13-7-12-21(2)3)16-8-5-6-9-19(16)24-20/h5-6,8-11,14H,4,7,12-13H2,1-3H3
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| Chemical Name |
1-[10-[3-(dimethylamino)propyl]phenothiazin-2-yl]propan-1-one
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (293.70 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 | 2.9370 mL | 14.6852 mL | 29.3703 mL | |
| 5 mM | 0.5874 mL | 2.9370 mL | 5.8741 mL | |
| 10 mM | 0.2937 mL | 1.4685 mL | 2.9370 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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