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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.
分子量 | 412.33 |
公式 | C21H23ClFNO2.HCl |
储存 | Store at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 10.31 | 25 温和加热 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 Haloperidol hydrochloride 的部分引用包括:
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
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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.