Ziprasidone HCl hydrate

Ziprasidone HCl hydrate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 330104

CAS#: 138982-67-9 (HCl hydrate)

Description: Ziprazidone is approved for the treatment of schizophrenia, and acute mania and mixed states associated with bipolar disorder. Its intramuscular injection form is approved for acute agitation in schizophrenic patients for whom treatment with just ziprasidone is appropriate. The mechanism of action of ziprasidone, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug's efficacy in schizophrenia is mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5HT2) antagonism. As with other drugs having efficacy in bipolar disorder, the mechanism of action of ziprasidone in bipolar disorder is unknown.

Chemical Structure

Ziprasidone HCl hydrate

CAS# 138982-67-9 (HCl hydrate)

Instruction

Theoretical Analysis

MedKoo Cat#: 330104
Name: Ziprasidone HCl hydrate
CAS#: 138982-67-9 (HCl hydrate)
Chemical Formula: C21H24Cl2N4O2S
Exact Mass: 0.00
Molecular Weight: 467.409
Elemental Analysis: C, 53.96; H, 5.18; Cl, 15.17; N, 11.99; O, 6.85; S, 6.86

Price and Availability

Size	Price	Availability
100mg	USD 250	2 weeks
250mg	USD 450	2 weeks
500mg	USD 650	2 Weeks
1g	USD 950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Ziprasidone HCl hydrate; CP88059; CP-88059; CP 88059; CP-88,059; CP-88,059-01; CP88059 hydrochloride; Ziprasidone HCl,

IUPAC/Chemical Name: 5-[2-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one Hydrochloride Monohydrate

InChi Key: ZCBZSCBNOOIHFP-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H21ClN4OS.ClH.H2O/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;1H2

SMILES Code: O=C1NC2=C(C=C(CCN3CCN(C4=NSC5=C4C=CC=C5)CC3)C(Cl)=C2)C1.[H]Cl.[H]O[H]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 467.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Bouchette D, Pellegrini MV. Ziprasidone. 2017 Oct 9. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2017 Jun-. Available from http://www.ncbi.nlm.nih.gov/books/NBK448157/ PubMed PMID: 28846230.

2: Mandrioli R, Protti M, Mercolini L. Evaluation of the pharmacokinetics, safety and clinical efficacy of ziprasidone for the treatment of schizophrenia and bipolar disorder. Expert Opin Drug Metab Toxicol. 2015 Jan;11(1):149-74. doi: 10.1517/17425255.2015.991713. Epub 2014 Dec 6. Review. PubMed PMID: 25483358.

3: Lee HB, Yoon BH, Kwon YJ, Woo YS, Lee JG, Kim MD, Bahk WM. The efficacy and safety of switching to ziprasidone from olanzapine in patients with bipolar I disorder: an 8-week, multicenter, open-label study. Clin Drug Investig. 2013 Oct;33(10):743-53. doi: 10.1007/s40261-013-0120-y. Review. PubMed PMID: 23990283.

4: Andrade C. Antidepressant action of atypical antipsychotics: focus on ziprasidone monotherapy, with a few twists in the tale. J Clin Psychiatry. 2013 Mar;74(3):e193-6. doi: 10.4088/JCP.13f08410. Review. PubMed PMID: 23561239.

5: Pappadopulos E, Newcomer JW, Kolluri S. Changes in weight, plasma lipids, and glucose in adults treated with ziprasidone: a comprehensive analysis of pfizer-initiated clinical trials. J Clin Psychiatry. 2012 Jun;73(6):e742-8. doi: 10.4088/JCP.10r06802. Review. PubMed PMID: 22795213.

6: Stip E, Zhornitsky S, Moteshafi H, Létourneau G, Stikarovska I, Potvin S, Tourjman V. Ziprasidone for psychotic disorders: a meta-analysis and systematic review of the relationship between pharmacokinetics, pharmacodynamics, and clinical profile. Clin Ther. 2011 Dec;33(12):1853-67. doi: 10.1016/j.clinthera.2011.10.027. Epub 2011 Dec 1. Review. PubMed PMID: 22133697.

7: Sacchetti E, Galluzzo A, Valsecchi P. Oral ziprasidone in the treatment of patients with bipolar disorders: a critical review. Expert Rev Clin Pharmacol. 2011 Mar;4(2):163-79. doi: 10.1586/ecp.10.139. Review. PubMed PMID: 22115400.

8: Cañas F, Correll CU, Fagiolini A, Larmo I, Levy P, Papageorgiou G, Rossi A, Zink M, Montes JM. Practical guidance for prescribing ziprasidone in acute manic or mixed episodes of bipolar I disorder. Expert Opin Pharmacother. 2011 Oct;12(14):2245-63. doi: 10.1517/14656566.2011.605787. Epub 2011 Jul 30. Review. PubMed PMID: 21801083.

9: Ochedzan D, Jarema M. [Practical aspects of the use of ziprasidone in schizophrenia]. Psychiatr Pol. 2010 Nov-Dec;44(6):881-93. Review. Polish. PubMed PMID: 21449170.

10: Citrome L. Drug safety evaluation of ziprasidone. Expert Opin Drug Saf. 2011 May;10(3):437-48. doi: 10.1517/14740338.2011.560114. Epub 2011 Feb 19. Review. PubMed PMID: 21332416.

11: Fagiolini A, Cañas F, Gallhofer B, Larmo I, Levy P, Montes JM, Papageorgiou G, Zink M, Rossi A. Strategies for successful clinical management of schizophrenia with ziprasidone. Expert Opin Pharmacother. 2010 Sep;11(13):2199-220. doi: 10.1517/14656566.2010.507630. Review. PubMed PMID: 20658947.

12: Citrome L. Ziprasidone HCl capsules for the adjunctive maintenance treatment of bipolar disorder in adults. Expert Rev Neurother. 2010 Jul;10(7):1031-7. doi: 10.1586/ern.10.66. Review. PubMed PMID: 20586686.

13: Khan AA, Strawn JR, Croarkin PE. Emerging treatment options in bipolar disorder in adolescents: focus on ziprasidone. Adolesc Health Med Ther. 2010 Oct 11;1:137-43. doi: 10.2147/AHMT.S7586. eCollection 2010. Review. PubMed PMID: 24600269; PubMed Central PMCID: PMC3915792.

14: Komossa K, Rummel-Kluge C, Hunger H, Schwarz S, Bhoopathi PS, Kissling W, Leucht S. Ziprasidone versus other atypical antipsychotics for schizophrenia. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD006627. doi: 10.1002/14651858.CD006627.pub2. Review. PubMed PMID: 19821380; PubMed Central PMCID: PMC4164848.

15: Citrome L. Using oral ziprasidone effectively: the food effect and dose-response. Adv Ther. 2009 Aug;26(8):739-48. doi: 10.1007/s12325-009-0055-0. Epub 2009 Aug 8. Review. PubMed PMID: 19669631.

16: Rosa AR, Franco C, Torrent C, Comes M, Cruz N, Horga G, Benabarre A, Vieta E. Ziprasidone in the treatment of affective disorders: a review. CNS Neurosci Ther. 2008 Winter;14(4):278-86. doi: 10.1111/j.1755-5949.2008.00056.x. Review. PubMed PMID: 19040553.

17: Durán-Ferreras E, Alvarez-López M, García-Moreno JM, Chacón J. [Ziprasidone in Parkinsonian dopamine psychosis]. Rev Neurol. 2008 Apr 16-30;46(8):476-80. Review. Spanish. PubMed PMID: 18428105.

18: Preskorn SH. Clinical relevance of relative receptor binding affinity: quetiapine and ziprasidone as examples. J Psychiatr Pract. 2007 Nov;13(6):393-8. Review. PubMed PMID: 18032984.

19: Warrington L, Lombardo I, Loebel A, Ice K. Ziprasidone for the treatment of acute manic or mixed episodes associated with bipolar disorder. CNS Drugs. 2007;21(10):835-49. Review. PubMed PMID: 17850172.

20: Greenberg WM, Citrome L. Ziprasidone for schizophrenia and bipolar disorder: a review of the clinical trials. CNS Drug Rev. 2007 Summer;13(2):137-77. Review. PubMed PMID: 17627670.

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