cis-Flupenthixol (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki: 0.38 nM for dopamine D2 receptors
Cis-Flupenthixol is an antagonist at dopamine D2 receptors.
Dopamine receptor D2 is encoded by the DRD2 gene. It has been suggested that dopamine receptors are the action site of antipsychotic drugs. The dopamine D2 receptor is also the main receptor for all antipsychotic drugs.
In vitro: The effects of striatal kainic acid lesions on [3H] cis-flupenthixol and [3H]spiperone binding to dopamine receptors were examined in a previous study. Significant reductions in both binding parameters were observed, and [3H] cis-flupenthixol binding was depleted to a greater level than [3H]spiperone binding. Reductions in both binding were correlated with reductions in glutamic acid decarboxylase activity [1].
In vivo: In a previous animal study rats were conditioned to associate an environment with immediate or delayed effects of pre-treatment with either cis-flupenthixol or saline vehicle. Results showed that vehicle-treated control animals developed the normal pattern of CPPs and cis-flupenthixol-caused DA receptor antagonism could prevent the expression of cocaine CPPs but it did not alter the expression of cocaine-induced CPAs [2].
Clinical trial: Clinical study found that the greatest deterioration in patients reduced from above to below 200 mg cis(z)-flupenthixol decanoate. A examinatioin of all the patients showed a relationship between deterioration of schizophrenic and depressive features and cis(z)-flupenthixol plasma levels. Side-effects were few, and no emergence of tardive dyskinesia was observed [3].
References:
[1] Cross AJ, Waddington JL. Kainic acid lesions dissociate [3H] spiperone and [3H]cis-flupenthixol binding sites in rat striatum. Eur J Pharmacol. 1981 May 8;71(2-3):327-32.
[2] Wenzel JM, Su ZI, Shelton K, Dominguez HM, von Furstenberg VA, Ettenberg A. The dopamine antagonist cis-flupenthixol blocks the expression of the conditioned positive but not the negative effects of cocaine in rats. Pharmacol Biochem Behav. 2013 Dec;114-115:90-6.
[3] Cookson IB. The effects of a 50% reduction of cis(z)-flupenthixol decanoate in chronic schizophrenic patients maintained on a high dose regime. Int Clin Psychopharmacol. 1987 Apr;2(2):141-9.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 507.4 |
Cas No. | 51529-01-2 |
Formula | C23H25F3N2OS·2HCl |
Synonyms | cis-Flupentixol |
Solubility | ≤1mg/ml in ethanol;25mg/ml in DMSO;15mg/ml in dimethyl formamide |
Chemical Name | 4-[3-[(3Z)-2-(trifluoromethyl)-9H-thioxanthen-9-ylidene]propyl]-1-piperazineethanol, dihydrochloride |
SDF | Download SDF |
Canonical SMILES | OCCN(CC1)CCN1CC/C=C2C3=C(C=CC(C(F)(F)F)=C3)SC4=CC=CC=C4\2.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |