intermediate of ziprasidone | intermediate of ziprasidone: 5-(2-chloroethyl) -6-chloro-1, 3-dihydro-indol-2-(2H)-One, 5-chloroacetyl-6-chloro-1, 3-dihydro-2h-indol-2-one, 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride is a kind of atypical antipsychotic drugs, belongs to benzothiazole piperazine compounds, in vitro, this product on dopamine D2, D3, 5-HT2A, 5-HT2C, 5-HT1A, the affinity of 5-HT1D and α1 adrenoceptors is strong; The affinity for histamine H1 receptors is moderate. It has antagonistic effect on dopamine D1, D2, 5-HT2A, 5-HT1D and agonistic effect on 5-HT1A receptor. This product inhibits the reuptake of 5-HT and norepinephrine by presynaptic membrane. The mechanism of action is not clear, it may be through the combined antagonism of dopamine D2 and 5-HT2 to produce anti schizophrenia effect, its blocking intensity is similar to risperidone and haloperidol, and is stronger than olanzapine, quetiapine and clozapine, mainly used for acute or chronic, primary or recurrent schizophrenia, schizophrenia negative, positive symptoms are effective. In particular, the effect of negative symptoms is better. It can reduce hallucinations, delusions, thinking and abnormal action and other positive symptoms; But also improve the emotional monotony, the will of the sex to reduce the negative symptoms. Atypical antipsychotic drugs, also known as a new generation of antipsychotic drugs, refers to the dopamine D2 receptor blocking is weaker than the 5-HT2A receptor blocking antipsychotic drugs, such as the current clinical use of clozapine, concomitant ketones, olanzapine, quetiapine, ziprasidone and other drugs are such. Atypical antipsychotics in addition to clinical application of clozapine earlier (70 years). Atypical antipsychotics not only block dopamine D2 receptors, but also have a stronger effect of blocking 5-HT2A receptors. When blocking the midbrain-limbic pathway dopamine D2 receptors, can improve the patient's positive symptoms; When blocking the midbrain-cortical pathway on the presynaptic membrane of 5-HT2A receptors, can cause the release of dopamine, excites dopamine D1 receptor in dorsolateral prefrontal cortex, improves negative and cognitive symptoms, excites dopamine D1 receptor in medial prefrontal cortex and orbit, and improves depressive symptoms; when blocking 5-HT2A receptors on the presynaptic membrane of the substantia nigra-striatal pathway causes a deinhibitory release of dopamine, which may partially counteract the blockade of dopamine D2 receptors by the drug, so the extrapyramidal reaction is mild (long-term use is not easy to cause tardive dyskinesia); When the 5-HT2A receptor on the presynaptic membrane of the hypothalamus-infundibulum is blocked, the deinhibitory release of dopamine is caused, which partially counteracts the blockade of the dopamine D2 receptor by the drug, so that Hyperprolactinemia is not obvious. |