10457-90-6

Usage

Uses

Used in Pharmaceutical Industry:
BROMPERIDOL is used as an antipsychotic agent for the treatment of various psychiatric disorders. It helps in managing symptoms such as hallucinations, delusions, and agitation associated with conditions like schizophrenia and bipolar disorder.
Used in Pain Management:
BROMPERIDOL is used as an analgesic to alleviate pain. Its effectiveness in pain relief can be beneficial for patients suffering from acute or chronic pain conditions.
Used in Inflammation Reduction:
BROMPERIDOL is also used as an anti-inflammatory agent, which can help in reducing inflammation and associated discomfort in various medical conditions.

InChI:InChI=1/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

Upstream product

• 3874-54-2 4-(4-fluorophenyl)-4-oxo-n-butyl chloride 
• 57988-58-6 4-(4-bromophenyl)-4-hydroxy-piperidine 
• 114361-10-3 4-<4-hydroxy-4-(4-aminophenyl)piperidinyl>-1-(4-fluorophenyl)butanone 
• 97042-48-3 4-<4-<4-(trimethylstannyl)phenyl>-4-hydroxypiperidino>-4'-fluorobutyrophenone 

Downstream Products

• 366-77-8 4-(4-fluorophenyl)-4-oxopropionic acid 

Related news

Comparison of prolactin concentrations between haloperidol and BROMPERIDOL (cas 10457-90-6) treatments in schizophrenic patients08/03/2019

The antipsychotic drug, bromperidol, is a close structural analogue of haloperidol. These two drugs also have similarities in metabolic pathways and pharmacological properties. In the present study, the prolactin concentrations in plasma during bromperidol versus haloperidol treatments were comp...detailed

Repurposing antipsychotic drugs into antifungal agents: Synergistic combinations of azoles and BROMPERIDOL (cas 10457-90-6) derivatives in the treatment of various fungal infections07/31/2019

As the number of hospitalized and immunocompromised patients continues to rise, invasive fungal infections, such as invasive candidiasis and aspergillosis, threaten the life of millions of patients every year. The azole antifungals are currently the most prescribed drugs clinically that display ...detailed

Relevant academic research and scientific papers

Repurposing antipsychotic drugs into antifungal agents: Synergistic combinations of azoles and bromperidol derivatives in the treatment of various fungal infections

As the number of hospitalized and immunocompromised patients continues to rise, invasive fungal infections, such as invasive candidiasis and aspergillosis, threaten the life of millions of patients every year. The azole antifungals are currently the most prescribed drugs clinically that display broad-spectrum antifungal activity and excellent oral bioavailability. Yet, the azole antifungals have their own limitations and are unable to meet the challenges associated with increasing fungal infections and the accompanied development of resistance against azoles. Exploring combination therapy that involves the current azoles and another drug has been shown to be a promising strategy. Haloperidol and its derivative, bromperidol, were originally discovered as antipsychotics. Herein, we synthesize and report a series of bromperidol derivatives and their synergistic antifungal interactions in combination with a variety of current azole antifungals against a wide panel of fungal pathogens. We further select two representative combinations and confirm the antifungal synergy by performing time-kill assays. Furthermore, we evaluate the ability of selected combinations to destroy fungal biofilm. Finally, we perform mammalian cytotoxicity assays with the representative combinations against three mammalian cell lines.

Synthesis of High Specific Activity - and Bromperidol and Tissue Distribution Studies in the Rat

A rapid synthesis of - and bromperidol with specific activity exceeding 10 000 Ci/mmol is described in which a trimethylstannylated analogue of bromperidol is used as a substrate for regiospecific no-carrier-added radiobromination. 4--4-hydroxypiperidino>-4'-fluorobutyrophenone was synthesized by the reaction of (trimethylstannyl)sodium with haloperidol and purified by preparative HPLC.Subsequent radiobromination with no-carrier-added 75Br- or 77Br- and in situ oxidation using H2O2/CH3COOH gave a corrected radiochemical yield of 35percent with a 30-min preparation time.Tissue distribution studies in the rat show a rapid and prolonged uptake into the brain, liver, and kidneys and consistently low blood concentrations that differ quantitatively from previous studies using relatively low specific activity bromperidol.Potential clinical applications for this high specific activity radiobrominated neuroleptic are discussed.

Antifungal Compositions

Provided herein are antifungal compositions and methods of use thereof. The antifungal compositions include an antifungal agent and an antipsychotic agent or an antihistamine. The methods of use thereof include administering a composition including an antifungal agent and an antipsychotic or an antihistamine to a plant or animal in need thereof.

Synthesis of [82Br]bromperidol and preliminary tissue distribution studies in the rat.

A procedure is described for the preparation of [82Br]bromperidol with specific activity 440 muCi/mg. The incorporation of bromine-82 into the molecule was accomplished through Brackman and Smit's modification of the Sandmeyer reaction, during the last step of the synthetic route. This involved the formation of a complex between Cu82Br2 and nitric oxide gas in acetonitrile, which was then allowed to react with 4-[4-(aminophenyl)-4-hydroxy-piperidinyl]-1-(4-fluorophenyl)-1-butanone (aminoperidol, 10) to give [82Br]bromperidol in about 1.5 h. Cupric 82Br]bromide was prepared in situ from K82Br and CuSO4.5H2O. The radiochemical and chemical yields for the preparation of [82Br]bromperidol from K82Br were 10.4 and 12%, respectively. Preliminary tissue distribution studies with the labeled bromperidol in the rat showed that the uptake of radioactivity by the liver, brain, kidneys, and the lungs was very fast and was in the declining phase in the latter organs 15 min after iv administration.