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Haloperidol

Haloperidol is a butyrophenone antipsychotic that is clinically used to treat psychosis, obsessive-compulsive disorder, and various other personality disorders. Haloperidol acts as an antagonist at D2 receptors, α1-adrenergic receptors, 5-HT2A receptors, and σ1 receptors; it also activates σ2 receptors.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18930088

Cas No.

52-86-8

Purity

≥95%

Formula

C21H23ClFNO2

Formula Wt.

375.86

Chemical Name

1-Butanone, 4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-

IUPAC Name

4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one

Synonym

Haldol; Halosten; Linton; Keselan; Aloperidin; Brotopon; Dozic.

Melting Point

148-149.4°C

Solubility

Soluble in chloroform, ethanol (16 mg/mL),methanol, acetone or benzene. Insoluble in water.

Appearance

White Crystal Powder

Cobos EJ, del Pozo E, Baeyens JM. Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells. J Neurochem. 2007 Aug;102(3):812-25. PMID: 17419803.

Colabufo NA, Berardi F, Contino M, et al. Antiproliferative and cytotoxic effects of some sigma2 agonists and sigma1 antagonists in tumour cell lines. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):106-13. PMID: 15322732.

Seeman P, Tallerico T. Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol Psychiatry. 1998 Mar;3(2):123-34. PMID: 9577836.

Schotte A, Janssen PF, Megens AA, et al. Occupancy of central neurotransmitter receptors by risperidone, clozapine and haloperidol, measured ex vivo by quantitative autoradiography. Brain Res. 1993 Dec 24;631(2):191-202. PMID: 7510574.

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