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Submit ReviewHaloperidol hydrochloride is a 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.
M. Wt | 412.33 |
Formula | C21H23ClFNO2.HCl |
Storage | Store at RT |
Purity | ≥98% (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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 10.31 | 25 with gentle warming |
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.
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 |
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.
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
Citations are publications that use Tocris products. Selected citations for Haloperidol hydrochloride include:
Kim et al (2012) Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun 426 177 PMID: 22925888
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
Balu et al (2008) Differential regulation of central BDNF protein levels by antidepressant and non-antidepressant drug treatments. Brain Res 1211 37 PMID: 18433734
Joshi and Panicker (2019) Identifying the In Vivo Cellular Correlates of Antipsychotic Drugs. Eneuro 5 PMID: 30713996
Oliver and Davies (2009) Interaction between environmental and genetic factors modulates schizophrenic endophenotypes in the Snap-25 mouse mutant blind-drunk. Hum Mol Genet 18 4576 PMID: 19729413
Kurita et al (2012) HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity. Nat Neurosci 15 1245 PMID: 22864611
Canfrán-Duque et al (2015) Curcumin Mitigates the Intracellular Lipid Deposit Induced by Antipsychotics In Vitro. Biochem J 10 e0141829 PMID: 26517556
Mishra et al (2015) Theσ-1 receptors are present in monomeric and oligomeric forms in living cells in the presence and absence of ligands. Brain Res 466 263 PMID: 25510962
Czysz et al (2015) Lateral diffusion of Gαs in the plasma membrane is decreased after chronic but not acute antidepressant treatment: role of lipid raft and non-raft membrane microdomains. J Biomol Screen 40 766 PMID: 25249058
Do you know of a great paper that uses Haloperidol hydrochloride from Tocris? Please let us know.
Average Rating: 5 (Based on 1 Review.)
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Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
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