化学性质：                                                                                                             

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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].

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