| CAS NO: | 51529-01-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 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 |
| 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 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
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.
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