| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
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| 100mg | |||
| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
D2 Receptor
Dopamine D2 receptors. Bromperidol is a potent antagonist of the dopamine D2 receptor. It also has affinity for other receptors, including dopamine D1, serotonin 5-HT2A, and alpha-1 adrenergic receptors. Its antipsychotic effect is primarily attributed to its D2 receptor antagonism in the mesolimbic and mesocortical pathways. |
|---|---|
| ln Vitro |
Bromperidol prevents conditioned responses and learned intracranial self-stimulation, and it opposes stereotyped behavior and agitation brought on by apomorphine or amphetamine in rats[1].
Bromperidol inhibits the conditioned avoidance response in dogs and counteracts the emesis caused by apomorphine[1]. Bromperidol potently inhibits dopamine D2 receptor-mediated signaling in vitro. In receptor binding assays, it has a high affinity for the D2 receptor. In functional assays, it can block the effects of dopamine, such as the inhibition of adenylate cyclase. |
| ln Vivo |
Bromoperidol can antagonize stereotyped behaviors and agitation induced by apomorphine or amphetamine, and inhibit conditioned responses and learned intracranial self-stimulation in rats [1]. Bromperidol antagonizes apomorphine-induced vomiting and inhibits the conditioned avoidance response in dogs [1].
In vivo, bromperidol is used for the treatment of schizophrenia and other psychotic disorders. It reduces positive symptoms such as hallucinations and delusions. Its long duration of action allows for once-daily or less frequent dosing. |
| Enzyme Assay |
In vitro receptor binding assays for bromperidol involve measuring its affinity for dopamine D2 and other receptors using radioligand binding techniques. Membranes from cells expressing the receptors are incubated with radiolabeled ligands and increasing concentrations of bromperidol. Ki values are determined.
|
| Cell Assay |
Cellular assays for bromperidol involve treating cells expressing dopamine D2 receptors with the compound and measuring its effects on receptor-mediated signaling, such as the inhibition of cAMP accumulation.
|
| Animal Protocol |
In vivo animal studies for bromperidol typically involve administration to animal models of psychosis. Efficacy is assessed by measuring behavioral endpoints such as locomotor activity and conditioned avoidance response.
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Bromopiperidine alcohol's known human metabolites include 4-(4-bromophenyl)piperidine-4-ol and 4'-fluorobutyrophenone. Bromperidol is well absorbed after oral and intramuscular administration. It has a long half-life, allowing for once-daily or less frequent dosing. The compound is metabolized in the liver and excreted in urine and feces. |
| Toxicity/Toxicokinetics |
Preclinical toxicity studies of bromperidol have established its safety profile. Common adverse effects include extrapyramidal symptoms, sedation, and weight gain. The compound is contraindicated in patients with a history of hypersensitivity to butyrophenones.
|
| References |
|
| Additional Infomation |
Bromperidol is an aromatic ketone. Bromperidol has been used in trials to treat dementia, depression, schizophrenia, anxiety disorders, and psychosomatic illnesses.
Bromperidol (Impromen) is a typical antipsychotic belonging to the butyrophenone class. It is a potent dopamine D2 receptor antagonist used for the treatment of schizophrenia and other psychotic disorders. It has a long duration of action and is available in oral and injectable formulations. |
| Molecular Formula |
C21H23BRFNO2
|
|---|---|
| Molecular Weight |
420.31522
|
| Exact Mass |
419.09
|
| Elemental Analysis |
C, 60.01; H, 5.52; Br, 19.01; F, 4.52; N, 3.33; O, 7.61
|
| CAS # |
10457-90-6
|
| Related CAS # |
Bromperidol hydrochloride; 59453-24-6; Bromperidol-d4-1
|
| PubChem CID |
2448
|
| Appearance |
Solid powder
|
| Density |
1.366 g/cm3
|
| Boiling Point |
543.6ºC at 760 mmHg
|
| Melting Point |
156-158ºC
|
| Flash Point |
282.6ºC
|
| Vapour Pressure |
1.19E-12mmHg at 25°C
|
| Index of Refraction |
1.59
|
| LogP |
4.472
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
451
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=C(F)C=C1)CCCN2CCC(O)(C3=CC=C(Br)C=C3)CC2
|
| InChi Key |
RKLNONIVDFXQRX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H23BrFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2
|
| Chemical Name |
4-[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
|
| Synonyms |
R-11333; R 11333; R11333; Impromen
|
| 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 |
| 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: ~50 mg/mL (~119 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 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 25.0 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: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3791 mL | 11.8957 mL | 23.7914 mL | |
| 5 mM | 0.4758 mL | 2.3791 mL | 4.7583 mL | |
| 10 mM | 0.2379 mL | 1.1896 mL | 2.3791 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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