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Ziprasidone
Ziprasidone

Ziprasidone

Price USD1.00
Packge 1KG
  • Min. Order:1G
  • Supply Ability:100KG
  • Time:2019-07-06

Product Details

  • Product NameZiprasidone
  • CAS No.146939-27-7
  • EINECS No.203-794-9
  • MFC21H21ClN4OS
  • MW412.94
  • AppearanceSolidBrown to Dark Brown
  • Melting point 213-215°C
  • storage temp. Sealed in dry,Room Temperature
  • Boiling point 554.8±50.0 °C(Predicted)
  • density 1.369±0.06 g/cm3(Predicted)

AD68

Ziprasidone Basic information
Atypical antipsychotic Dosage and usage Uses Production method
Product Name: Ziprasidone
Synonyms: Ziprasidone HBr;5-{2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl}-6-chloro-2,3-dihydro-1H-indol-2-one;Geodon;Ziprasidone solution;5-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one;ZIPRASIDONE-D8;5-[2-[4-(1,2-Benzisothiazol-3yl)-1-piperazinyl-d8]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one;2H-Indol-2-one, 5-2-4-(1,2-benzisothiazol-3-yl)-1-piperazinylethyl-6-chloro-1,3-dihydro-
CAS: 146939-27-7
MF: C21H21ClN4OS
MW: 412.94
EINECS: 203-794-9
Product Categories: Isotope Labelled Compounds;Sulfur & Selenium Compounds;API;Geodon, Zeldox;Other APIs;Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Isotope Labeled Compounds;Pharmaceuticals;Heterocycles
Mol File: 146939-27-7.mol
Ziprasidone Structure
 
Ziprasidone Chemical Properties
Melting point  213-215°C
storage temp.  Refrigerator
Merck  14,10171
CAS DataBase Reference 146939-27-7(CAS DataBase Reference)
 
Safety Information
Hazard Codes  F,T
Risk Statements  60-61-11-19-38
Safety Statements  53-45
RTECS  NM3241000
MSDS Information
 
 
Ziprasidone Usage And Synthesis
Atypical antipsychotic Ziprasidone is an atypical antipsychotic and belongs to piperazine benzothiazole compound. For in vitro condition, the product has a very high affinity to the dopamine D2, D3, 5-HT2A, 5-HT2C, 5-HT1A, 5-HT1D and α1 adrenergic receptor while having a moderate affinity to the histamine H1 receptor. However, it has antagonistic effect on dopamine D1, D2, 5-HT2A, 5-HT1D receptor while having agonistic effect on the 5-HT1A receptor. The product is capable of inhibiting the reuptake of 5-HT and norepinephrine via presynaptic membrane with the underlying mechanism of action remaining unclear. It may exert its anti-schizophrenia efficacy through the combined antagonist effect on dopamine D2 and 5-HT2 with the blocking strength being comparable to risperidone and haloperidol but stronger than olanzapine, quetiapine and clozapine. It is mainly used for the treatment of acute or chronic, onset or recurrent schizophrenia and is effective in treating both the negative as well as the positive symptoms of schizophrenia with especially a better efficacy in treating negative symptoms. It can reduce hallucinations, delusions, thought and action abnormal positive symptoms as well as alleviate the symptoms of mood monotonous and reduced volition activity and other negative symptoms. Atypical antipsychotics, also known as the new generation of antipsychotics, refers to a class of antipsychotics drug with its blockage effect on dopamine D2 receptor be weaker than its blockage effect on the 5-HT2A receptor. Clinical drugs at present such as clozapine, risperidone, olanzapine, quetiapine and ziprasidone all belongs to this category. For atypical antipsychotics, except clozapine which has a relative long history of clinical application (1970s), all these other drugs are new antipsychotics which did not emerge until the late 1990s. 
Atypical antipsychotics can not only block dopamine D2 receptors, but also more strongly block the effect of 5-HT2A receptor. When blocking the dopamine D2 receptor of midbrain-margin, it can also alleviate the positive symptoms; when blocking the 5-HT2A receptor on the presynaptic membrane of brain-cortical pathway, it can cause de-repressive release of dopamine and stimulate the dorsolateral dopamine D1 receptor of prefrontal cortex, alleviating the negative and cognitive symptoms, leading to excitement of the AVDM dopamine D1 receptors in the prefrontal cortex and the orbital part, further improving the symptoms of depression; when blocking the 5-HT2A receptor of the presynaptic membrane of the nigra-striatum pathway, it can cause the 5-HT2A receptor membranes, causing the de-repressive release of dopamine and can partially neutralizing the blocking effect of the drugs on the dopamine D2 receptor, therefore the extrapyramidal reactions are mild (long-term administration are also not easy to cause tardive dyskinesia); when causing blockage of the 5-HT2A receptor in the presynaptic membrane of the hypothalamic-funnel portion, it can cause de-repressive release of the dopamine, partially neutralizing the blocking effect of the drugs on the dopamine D2 receptor, therefore there is no obvious symptoms of hyperprolactinemia. It includes clozapine, olanzapine, quetiapine and ziprasidone.
Dosage and usage The initial dose is 2 times per day with 20mg each time through oral administration. The bioavailability is usually bioavailability 30% with administration together with food being able to double the absorption of this product, reaching the bioavailability of 60%; administration with high-fat meal together can make the bioavailability be up to 97%. Adjustment of the dose can start at two days later, usually twice daily with the dose range being within 20~80mg and the maximum dose being 100mg. Patients of mild to moderate liver and kidney damage don’t need to adjust the dose. Ziprasidone is mainly metabolized in the liver with the metabolites being mainly excreted from the urine and partially discharged through fecal. The terminal T1/2 is about 7h.
The above information is edited by the chemicalbook of Dai Xiongfeng.
Uses It is a kind of antipsychotic and can be used as the antagonist of the dopamine D2-serotonin 5-HT2.
Production method 6-Chloro-1,3-dihydro-2H-indol-2-ketone (I) and bromoacetic acid can have acylation reaction under the action of polyphosphoric acid to give the compound (II). And then be stirred together with silicon hydride and triethyl trifluoroacetic acid at room temperature to give the compound (III). Finally, it can have reaction with N-(3-benzisothiazole-yl) piperazine in MIBK containing sodium carbonate to give the product.
Chemical Properties Tan Solid
Uses Labelled Ziprasidone, which is used as an antipsychotic. Combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
Uses Ziprasidone (Geodon, Zeldox) was the fifth atypical antipsychotic to gain FDA approval. In the United States, Ziprasidone is approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation i
Uses Labeled Ziprasidone, intended for use as an internal standard for the quantification of Ziprasidone by GC- or LC-mass spectrometry.
Definition ChEBI: A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.

Company Profile Introduction

Henan CoreyChem Co., Ltd, based on the original Zhengzhou Cote Chemical Research Institute, be brave in absorbing highly educated talents & overseas returnees; actively responded to Zhengzhou City High-tech Zone Government’s Special Care Policy, reorganized and founded in National University of Science and Technology Park, which is a high-tech, stock enterprise of high-end chemical Custom synthesis;The park was created by the People's Government of Henan Province, and proved by Ministry of Education and the National Science & Technology, taking the construction mode of "many college a park, and common development", mainly depends on Zhengzhou University and Henan University’s scientific research and talent advantage to set up Universities, scientific research institute and enterprise scientific research achievements transformation platform, to make high-tech enterprises incubate,  is the new high-tech talent gathering base, high and new technology industry enterprise radiation base, colleges and universities technological innovation base.
 
Henan Coreychem Co., Ltd, facing global High-tech pharmaceutical raw materials, high complex new type intermediates, fine chemicals custom synthesis, scale-up production and Rare chemicals trade. Corey have well-equipped machine, strong technical force and considerate marketing team service. We also have rich experience advantage in basic research, small scale process development, scale-up, industrial technology development & production and cost control.
 

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  • Since:2014-12-17
  • Address: No.967,15th Floor,Unit 7, Building 1, No.70 of DianChang Road, High-tech Development Zone, Zhengzho
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