| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
D2 Receptor
Propionylpromazine hydrochloride targets the dopamine receptor D2 (DRD2). By acting as an antagonist at this receptor, it blocks dopamine-mediated signaling pathways. This antagonism is the basis for its use in research on antipsychotic mechanisms and sedation pathways. |
|---|---|
| ln Vitro |
In cell-free receptor binding assays, Propionylpromazine hydrochloride demonstrates high affinity for the dopamine D2 receptor. It displaces radiolabeled D2 ligands, confirming its interaction with the receptor. Its activity as an antagonist is characterized by its ability to block D2 receptor activation. Cellular assays for Propionylpromazine hydrochloride involve the use of cells expressing the dopamine D2 receptor. The compound's antagonistic activity is assessed by its ability to inhibit dopamine-induced signaling, such as the inhibition of cAMP production. These assays confirm its potency and efficacy at the D2 receptor.
|
| ln Vivo |
In vivo, Propionylpromazine hydrochloride is used as a veterinary tranquilizer, demonstrating its ability to produce sedation and calmness in animals. Its antagonism of dopamine D2 receptors in the central nervous system is responsible for these effects. The compound has also been investigated for its potential in psychiatric and neurological research.
|
| Enzyme Assay |
Cell-free receptor binding assays for Propionylpromazine hydrochloride are performed using membrane preparations from cells expressing the dopamine D2 receptor. Radioligand displacement studies use [³H]spiperone or similar D2-selective ligands. Membranes are incubated with varying concentrations of the compound and the radioligand, followed by filtration and scintillation counting. Ki values are calculated from competition binding curves.
|
| Cell Assay |
Cellular assays for Propionylpromazine hydrochloride are conducted using cells stably expressing the dopamine D2 receptor. Cells are pre-incubated with the compound, then stimulated with a D2 agonist. Functional responses such as cAMP accumulation are measured. IC50 values are determined from concentration-response curves.
|
| Animal Protocol |
In vivo animal studies for Propionylpromazine hydrochloride are conducted in the context of its use as a veterinary tranquilizer. The compound is administered to animals, and its sedative and calming effects are observed. These studies confirm its pharmacological activity in a whole-organism context.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Propionylpromazine hydrochloride are characteristic of phenothiazine antipsychotics. It is well-absorbed and extensively metabolized in the liver. The compound's half-life and bioavailability are influenced by its lipophilic nature. Detailed PK parameters are available in veterinary pharmacology literature.
|
| Toxicity/Toxicokinetics |
Propionylpromazine hydrochloride can cause side effects related to its antagonism of dopamine D2 receptors, including sedation, extrapyramidal symptoms, and cardiovascular effects. Its use as a veterinary tranquilizer requires careful dosing to avoid adverse reactions. Comprehensive toxicological data are available in veterinary pharmacology references.
|
| References |
[1]. Tyers, Mike, et al. Method for treating a brain cancer with ifenprodil. US8058243.
|
| Additional Infomation |
Propionylpromazine hydrochloride is a veterinary tranquilizer and a research tool for studying dopaminergic signaling and antipsychotic mechanisms. It is also used in Parkinson's disease research. The compound is not approved for human use but is available for research purposes.
|
| Molecular Formula |
C20H25CLN2OS
|
|---|---|
| Molecular Weight |
376.94
|
| Exact Mass |
376.138
|
| CAS # |
7681-67-6
|
| Related CAS # |
Propionylpromazine;3568-24-9;Propionylpromazine-d6 hydrochloride;1262770-67-1
|
| PubChem CID |
24351
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
507.4ºC at 760 mmHg
|
| Melting Point |
90-93ºC
|
| Flash Point |
260.7ºC
|
| LogP |
5.7
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
25
|
| Complexity |
428
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCC(=O)C1=CC2=C(C=C1)SC3=CC=CC=C3N2CCCN(C)C.Cl
|
| InChi Key |
ZFWVWZODBGTOIL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H24N2OS.ClH/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;1H
|
| Chemical Name |
1-[10-[3-(dimethylamino)propyl]phenothiazin-2-yl]propan-1-one;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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, 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: 83.33 mg/mL (221.07 mM)
H2O: 8.33 mg/mL (22.10 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.52 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 (5.52 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: 50 mg/mL (132.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6529 mL | 13.2647 mL | 26.5294 mL | |
| 5 mM | 0.5306 mL | 2.6529 mL | 5.3059 mL | |
| 10 mM | 0.2653 mL | 1.3265 mL | 2.6529 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
