| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Bromperidol HCl targets dopamine receptors, primarily the D₂ receptor subtype. As a typical antipsychotic, it acts as a potent antagonist at D₂ receptors in the mesolimbic and mesocortical pathways of the brain. By blocking D₂ receptors, bromperidol HCl reduces dopamine-mediated neurotransmission, which is thought to be hyperactive in schizophrenia and other psychotic disorders. The compound may also have affinity for other dopamine receptor subtypes (D₁, D₃, D₄) and for other receptors such as serotonin (5-HT₂A) and adrenergic (α₁) receptors, although its primary antipsychotic effects are mediated through D₂ receptor antagonism.
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| ln Vitro |
Bromperidol HCl exhibits potent dopamine D₂ receptor antagonist activity in vitro. In radioligand binding assays using membrane preparations from cells expressing dopamine D₂ receptors, bromperidol HCl displaces D₂-selective radioligands with high affinity. The compound inhibits dopamine-stimulated adenylyl cyclase activity in cells expressing D₂ receptors, which is a functional measure of D₂ receptor antagonism. Bromperidol HCl also inhibits the binding of other dopamine receptor radioligands, demonstrating its affinity for other dopamine receptor subtypes. Specific IC₅₀ values vary depending on the assay system and receptor subtype.
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| ln Vivo |
In addition to inhibiting conditioned responses and learnt intracranial self-stimulation in rats, bromoperidol hydrochloride can counteract stereotyped behaviors and agitation brought on by apomorphine or amphetamine [1]. In dogs, apomorphine-induced vomiting can be countered and the conditioned avoidance response can be inhibited by bromperidol hydrochloride [1].
Bromperidol HCl exhibits antipsychotic activity in vivo in animal models. In behavioral models of psychosis such as apomorphine-induced stereotypy or amphetamine-induced hyperactivity in rodents, bromperidol HCl inhibits these behaviors at doses consistent with its D₂ receptor antagonist activity. The compound also produces catalepsy in rodents, which is a measure of extrapyramidal side effect potential typical of typical antipsychotics. Bromperidol HCl has been used clinically as an antipsychotic agent for the treatment of schizophrenia and other psychotic disorders. |
| Enzyme Assay |
Non-cellular assays for bromperidol HCl typically involve measuring its binding affinity to dopamine receptors using radioligand binding assays. In a typical assay, membrane preparations from cells expressing the dopamine D₂ receptor are incubated with a D₂-selective radioligand (e.g., [³H]spiperone or [³H]raclopride) and varying concentrations of bromperidol HCl. After incubation, bound radioligand is separated from free radioligand by filtration or centrifugation, and radioactivity is counted. IC₅₀ values for displacement of the radioligand are calculated, and Kᵢ values are derived using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for bromperidol HCl typically involve measuring its effects on dopamine receptor-mediated signaling. Cells expressing dopamine D₂ receptors are treated with varying concentrations of bromperidol HCl and then stimulated with a dopamine receptor agonist. The inhibition of agonist-stimulated adenylyl cyclase activity or other downstream signaling events (e.g., ERK phosphorylation, β-arrestin recruitment) is measured. The potency of bromperidol HCl as a D₂ receptor antagonist is determined from the inhibition curves.
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| Animal Protocol |
In vivo animal studies for bromperidol HCl typically use rodent models to evaluate antipsychotic activity and side effect profiles. In a typical antipsychotic activity assay, rodents are administered bromperidol HCl via oral, intraperitoneal, or subcutaneous routes. Apomorphine-induced stereotypy or climbing behavior is assessed, and the ED₅₀ for inhibition of these behaviors is determined. Catalepsy is assessed using the bar test or the grid test to evaluate extrapyramidal side effect potential. The therapeutic index (ratio of cataleptic ED₅₀ to antipsychotic ED₅₀) is calculated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of bromperidol HCl are characteristic of butyrophenone antipsychotics. Following oral administration, the compound is absorbed and undergoes extensive first-pass metabolism in the liver. Bromperidol HCl is highly lipophilic and has a large volume of distribution, indicating extensive tissue distribution. The compound is metabolized in the liver via cytochrome P450-mediated oxidation and reduction, and metabolites are excreted primarily in the urine and feces. The elimination half-life of bromperidol is approximately 24-48 hours, similar to haloperidol. The compound is highly protein-bound (>90%) in plasma.
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| Toxicity/Toxicokinetics |
Toxicological data for bromperidol HCl are derived from its clinical use as an antipsychotic agent. Common adverse effects include extrapyramidal symptoms such as parkinsonism, akathisia, and dystonia, which are dose-dependent and related to D₂ receptor blockade in the nigrostriatal pathway. Other adverse effects include sedation, orthostatic hypotension, anticholinergic effects (dry mouth, blurred vision, constipation), and weight gain. Rare but serious adverse effects include neuroleptic malignant syndrome, tardive dyskinesia, and QT interval prolongation. Bromperidol HCl is contraindicated in patients with Parkinson's disease, dementia with Lewy bodies, and known hypersensitivity to butyrophenones.
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| References |
[1]. Benfield P, et al. Bromperidol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in psychoses. Drugs. 1988 Jun;35(6):670-84.
[2]. Ramón-García S, et al. Synergistic drug combinations for tuberculosis therapy identified by a novel high-throughput screen. Antimicrob Agents Chemother. 2011 Aug;55(8):3861-9. |
| Additional Infomation |
Bromperidol HCl is a research-grade compound intended for laboratory use only and is not approved for clinical use in many countries. Its CAS number is 59453-24-6. The primary applications of bromperidol HCl include research on schizophrenia and psychosis, studies of dopamine receptor pharmacology and signaling, and use as a reference standard in analytical and pharmaceutical research. The compound is structurally related to haloperidol and shares a similar pharmacological profile. Bromperidol HCl is also used in behavioral pharmacology research to study the mechanisms of antipsychotic drug action and extrapyramidal side effects.
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| Molecular Formula |
C21H24BRCLFNO2
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| Molecular Weight |
456.78
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| Exact Mass |
455.066
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| CAS # |
59453-24-6
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| Related CAS # |
Bromperidol;10457-90-6
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| PubChem CID |
164517260
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
451
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F.Cl
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| InChi Key |
XAYXCUZHMISKSM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23BrFNO2.ClH/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;1H
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| Chemical Name |
4-[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one;hydrochloride
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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, 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)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~218.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.47 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 | 2.1892 mL | 10.9462 mL | 21.8924 mL | |
| 5 mM | 0.4378 mL | 2.1892 mL | 4.3785 mL | |
| 10 mM | 0.2189 mL | 1.0946 mL | 2.1892 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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