Haloperidol hydrochloride

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Cat.No. 0931 - Haloperidol hydrochloride | C21H23ClFNO2.HCl | CAS No. 1511-16-6
Description: Dopamine antagonist; displays some D2 selectivity
Chemical Name: 4-[4-(4-Chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (9)
Reviews (1)
Literature (5)

Biological Activity

Dopamine antagonist with selectivity for D2-like receptors (Ki values are 1.2, ~ 7, 2.3, ~ 80 and ~ 100 nM for D2, D3, D4, D1 and D5 receptors respectively). Subtype-selective NMDA antagonist. Identified as targeting human host proteins that interact with SARS-CoV-2.

Technical Data

M. Wt 412.33
Formula C21H23ClFNO2.HCl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 1511-16-6
PubChem ID 11495267
InChI Key JMRYYMBDXNZQMH-UHFFFAOYSA-N
Smiles Cl.OC1(CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1)C1=CC=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 4.12 10 with gentle warming
DMSO 10.31 25 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 412.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 9.7 mL 48.5 mL 97.01 mL
1.25 mM 1.94 mL 9.7 mL 19.4 mL
2.5 mM 0.97 mL 4.85 mL 9.7 mL
12.5 mM 0.19 mL 0.97 mL 1.94 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Beresford and Ward (1987) Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis. Drugs 33 31 PMID: 3545764

IIyin et al (1996) Subtype-selective inhibition of N-MthD.-aspartate receptors by halope. Mol.Pharmacol. 50 1541 PMID: 8967976

Lynch and Gallagher (1996) Inhibition of N-MthD.-aspartate receptors by haloperidol: development and pharmacological characterization in native and recombinant receptors. J.Pharmacol.Exp.Ther. 279 154 PMID: 8858988

Seeman and Van Tol (1994) DA receptor pharmacology. TiPS 15 264 PMID: 7940991

Merck Index 12 4629

Gordon et al (2020) A SARS-CoV-2 protein-protein interaction map reveals drug targets and drug repurposing. Nature 583 459 PMID: 32353859


If you know of a relevant reference for Haloperidol hydrochloride, please let us know.

View Related Products by Product Action

View all Non-selective Dopamine Antagonists

Keywords: Haloperidol hydrochloride, Haloperidol hydrochloride supplier, Antagonists, partly, D2-like, selective, High, affinity, ligands, σ1, sigma1, σ2, sigma2, antagonist, Dopamine, Non-Selective, Receptors, dopaminergic, COVID-19, SARS-CoV-2, severe, acute, respiratory, syndrome, Non-selective, Sigma1, 0931, Tocris Bioscience

⚠ WARNING: This product can expose you to chemicals including Haloperidol, which is known to the State of California to cause reproductive toxicity with developmental effects. For more information, go to www.P65Warnings.ca.gov

9 Citations for Haloperidol hydrochloride

Citations are publications that use Tocris products. Selected citations for Haloperidol hydrochloride include:

Watson et al (2012) The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Neuropsychopharmacology 1436 111 PMID: 22200378

Kim et al (2012) Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun 426 177 PMID: 22925888

Joshi and Panicker (2019) Identifying the In Vivo Cellular Correlates of Antipsychotic Drugs. Eneuro 5 PMID: 30713996

Kurita et al (2012) HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity. Nat Neurosci 15 1245 PMID: 22864611


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Reviews for Haloperidol hydrochloride

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Antagonist of D2R.
By Luiz Alexandre Magno on 10/26/2018
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: PC12 cells

I used haloperidol hydrochloride to block D2 dopamine receptors, which increases phosphorylation of the Akt protein (see the western blot image).

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