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Ziprasidone

Atypical antipsychotic Dosage and usage Uses Production method
Ziprasidone
Ziprasidone structure
CAS No.
146939-27-7
Chemical Name:
Ziprasidone
Synonyms
Geodon;CP 88059;Ziprasidone;ZIPRASIDONE-D8;Ziprasidone HBr;CP-88059:CP-88059-1;Ziprasidone solution;Hydrochloric acid(base);ZIPRASIDONE: ZIPRASIDONE HYDROCHLORIDE MONOHYDRATE;5-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one
CBNumber:
CB6167417
Molecular Formula:
C21H21ClN4OS
Formula Weight:
412.94
MOL File:
146939-27-7.mol

Ziprasidone Properties

Melting point:
213-215°C
Boiling point:
554.8±50.0 °C(Predicted)
Density 
1.369±0.06 g/cm3(Predicted)
storage temp. 
Refrigerator
pka
13.34±0.20(Predicted)
Merck 
14,10171
CAS DataBase Reference
146939-27-7(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
Hazard Codes  F,T
Risk Statements  60-61-11-19-38
Safety Statements  53-45
RTECS  NM3241000

Ziprasidone price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TCI Chemical Z0034 Ziprasidone >98.0%(HPLC) 146939-27-7 100mg $60 2018-11-22 Buy
TCI Chemical Z0034 Ziprasidone >98.0%(HPLC) 146939-27-7 1g $360 2018-11-22 Buy

Ziprasidone Chemical Properties,Uses,Production

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.

brand name

Geodon (Pfizer).

General Description

Ziprasidone (Geodon, a benzisothiazolpiprazinylindolonederivative) also has the structuralfeatures of a hybrid molecule between a butyrophenone antipsychoticand a trazodone-like antidepressant. It is highlymetabolized to four major metabolites, only one of which, Smethyldihydroziprasidone,likely contributes to its clinical activity. In humans, less than 5% of the dose isexcreted unchanged. Reduction by aldehyde oxidase accountsfor about 66% of ziprasidone metabolism; two oxidative pathwaysinvolving hepatic CYP3A4 account for the remainder.

General Description

Ziprasidone, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one, is available as the hydrochloride monohydrate for oral administration (Geodon) and as the mesylate trihydrate saltfor intramuscular (IM) injection. The compound is well absorbedwith peak plasma levels occurring at 6 to 8 hours afteroral administration. The oral absorption is enhanced approximatelytwofold in the presence of food. Ziprasidone isbound about 99% to plasma proteins, primarily to albuminand α1-acid glycoprotein. Ziprasidone is not displaced in thepresence of two highly protein bound drugs, warfarin andpropranolol. Ziprasidone is extensively metabolized withonly about 5 % of the drug excreted unchanged.23 In humans,two major pathways are responsible for the metabolism ofziprasidone: (a) oxidation by CYP3A4 (one third) and (b) reductionby aldehyde oxidase (two thirds).The combinedaction of these metabolic pathways leads to four majorcirculating metabolites: benzisothiazole piperazine sulfoxide(BITP-sulfoxide), benzisothiazole piperazine sulfone (BITPsulfone),ziprasidone sulfoxide, and S-methyldihydroziprasidone.

Ziprasidone Preparation Products And Raw materials

Raw materials

Preparation Products


Ziprasidone Suppliers

Global( 125)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21671 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sale@mainchem.com CHINA 32447 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30001 58
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23980 58
Xiamen AmoyChem Co., Ltd
+86 592-605 1114
sales@amoychem.com CHINA 6372 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 35440 58
Shanghai Boyle Chemical Co., Ltd.
86-21-57758967 sales@boylechem.com China 2926 55
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15881 69

View Lastest Price from Ziprasidone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-20 Ziprasidone
146939-27-7
US $1.00 / KG 1G 98% 100KG career henan chemical co
2018-07-27 Hydrochloric acid(base)
146939-27-7
US $100.00 / G 1G 985 50kg career henan chemical co

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