Size | Price | Stock | Qty |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Other Sizes |
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Purity: ≥98%
Ziprasidone (CP 88059; CP-88,059; CP-88,059-01; Geodon; Zeldox; Zipwell) HCl, the hydrochloride salt of Ziprasidone, is a novel and potent dopamine and serotonin (5-HT) receptor antagonist with antipsychotic effects. It is authorized for the treatment of acute mania, mixed states linked to bipolar disorder, and schizophrenia and bipolar illness. When treating schizophrenia patients who respond best to treatment consisting solely of ziprasidone, its intramuscular injection form is authorized for use in cases of acute agitation. According to theories about ziprasidone's mode of action, serotonin type 2 (5HT2) and dopamine type 2 (D2) antagonistic interactions together mediate the drug's effectiveness in treating schizophrenia. The exact mechanism by which ziprasidone treats bipolar disorder is unknown, as it is with other medications that are effective in treating the condition.
Targets |
Rat 5-HT2A ( Ki = 0.42 nM ); Rat 5-HT1A Receptor ( Ki = 3.4 nM ); Rat D2 Receptor ( Ki = 4.8 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
Cell Line: HEK-293 cells
Concentration: 0-500 nM Incubation Time: 150 seconds Result: Blocked wild-type hERG current in a voltage- and concentration-dependent manner (IC50 = 120 nm). |
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Animal Protocol |
Eight-week-old female Sprague-Dawley rats weighing 200 to 250 g
20 mg/kg Oral gavage; 20 mg/kg; once daily; 7 weeks |
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Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Because there is little published experience with ziprasidone during breastfeeding, other antipsychotic agents may be preferred, especially while nursing a newborn or preterm infant. A safety scoring system finds ziprasidone possible to use cautiously during breastfeeding. Infants breastfed during maternal use of ziprasidone should be monitored for excess sedation, irritability, poor feeding, and extrapyramidal symptoms, such as tremors and abnormal muscle movements. ◉ Effects in Breastfed Infants A woman took ziprasidone 40 mg and citalopram 60 mg daily throughout pregnancy and postpartum. She breastfed extensively, except for occasional formula feedings by others. At 6 months of age, a pediatrician found the infant to be healthy with normal growth and development. Patients enlisted in the National Pregnancy Registry for Atypical Antipsychotics who were taking a second-generation antipsychotic drug while breastfeeding (n = 576) were compared to control breastfeeding patients who were not treated with a second-generation antipsychotic (n = 818). Of the patients who were taking a second-generation antipsychotic drug, 60.4% were on more than one psychotropic. A review of the pediatric medical records, no adverse effects were noted among infants exposed or not exposed to second-generation antipsychotic monotherapy or to polytherapy. The number of women taking ziprasidone was not reported. ◉ Effects on Lactation and Breastmilk Prolactin elevation has occurred during ziprasidone treatment, and galactorrhea has been reported, often in adolescents. However, prolactin elevation might be more transient and less severe than with phenothiazines. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. Patients enlisted in the National Pregnancy Registry for Atypical Antipsychotics who were taking a second-generation antipsychotic drug while breastfeeding (n = 576) were compared to control breastfeeding patients who had primarily diagnoses of major depressive disorder and anxiety disorders, most often treated with SSRI or SNRI antidepressants, but not with a second-generation antipsychotic (n = 818). Among women on a second-generation antipsychotic, 60.4% were on more than one psychotropic compared with 24.4% among women in the control group. Of the women on a second-generation antipsychotic, 59.3% reported “ever breastfeeding” compared to 88.2% of women in the control group. At 3 months postpartum, 23% of women on a second-generation antipsychotic were exclusively breastfeeding compared to 47% of women in the control group. The number of women taking ziprasidone was not reported. |
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References | ||
Additional Infomation |
Ziprasidone Hydrochloride is the hydrochloride salt form of ziprasidone, a benzothiazolylpiperazine derivative and an atypical antipsychotic agent with an antischizophrenic property. Ziprasidone hydrochloride functions as an antagonist at the dopamine D2 and serotonin 5-HT2A and 5-HT1D receptors, and as an agonist at the 5-HT1A receptor. Ziprasidone hydrochloride also inhibits synaptic reuptake of serotonin and norepinephrine. The mechanism of action by which ziprasidone hydrochloride exerts its antischizophrenic effect is unknown but is potentially mediated through a combination of dopamine D2 and serotonin 5-HT2 antagonism. This agent also has antagonistic activity against histamine H1 and alpha-1-adrenergic receptors.
See also: Ziprasidone (has active moiety). |
Molecular Formula |
C21H22CL2N4OS
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Molecular Weight |
449.4
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Exact Mass |
448.089
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Elemental Analysis |
C, 56.13; H, 4.93; Cl, 15.78; N, 12.47; O, 3.56; S, 7.13
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CAS # |
122883-93-6
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Related CAS # |
Ziprasidone; 146939-27-7; Ziprasidone-d8; 1126745-58-1; Ziprasidone hydrochloride monohydrate; 138982-67-9; Ziprasidone mesylate trihydrate; 199191-69-0; Ziprasidone mesylate; 185021-64-1
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PubChem CID |
219099
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Appearance |
Solid powder
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LogP |
4.751
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Hydrogen Bond Donor Count |
2
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
4
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Heavy Atom Count |
29
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Complexity |
573
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Defined Atom Stereocenter Count |
0
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SMILES |
ClC1=CC2=C(CC(N2)=O)C=C1CCN(CC3)CCN3C4=NSC5=C4C=CC=C5.Cl
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InChi Key |
NZDBKBRIBJLNNT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H21ClN4OS.ClH/c22-17-13-18-15(12-20(27)23-18)11-14(17)5-6-25-7-9-26(10-8-25)21-16-3-1-2-4-19(16)28-24-21;/h1-4,11,13H,5-10,12H2,(H,23,27);1H
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Chemical Name |
5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one;hydrochloride
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2252 mL | 11.1259 mL | 22.2519 mL | |
5 mM | 0.4450 mL | 2.2252 mL | 4.4504 mL | |
10 mM | 0.2225 mL | 1.1126 mL | 2.2252 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
An Investigation of Sleep Architecture in Ziprasidone-Treated Bipolar Depression
CTID: NCT00835107
Phase: Phase 4   Status: Completed
Date: 2015-12-16