Ziprasidone hydrochloride monohydrate5-HT (serotonin)/dopamine receptor antagonist CAS# 138982-67-9 |
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Quality Control & MSDS
3D structure
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| Cas No. | 138982-67-9 | SDF | Download SDF |
| PubChem ID | 60853 | Appearance | Powder |
| Formula | C21H24Cl2N4O2S | M.Wt | 467.41 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | CP 88059 | ||
| Solubility | DMSO : 25 mg/mL (53.49 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one;hydrate;hydrochloride | ||
| SMILES | C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.O.Cl | ||
| Standard InChIKey | ZCBZSCBNOOIHFP-UHFFFAOYSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Atypical antipsychotic that displays combined serotonin and dopamine receptor antagonism. Displays high affinity at 5-HT2A receptors with a 5-HT2A/D2 affinity ratio greater than any other clinically available atypical antipsychotics (pKi values are 9.38, 8.88, 8.69, 8.47, 8.32, 8.14, 7.98, 7.49, 7.33 and 6.28 for 5-HT2A, 5-HT2C, 5-HT1D, 5-HT1A, D2, D3, α1, D4, H1 and D1 receptors respectively). |
Ziprasidone hydrochloride monohydrate Dilution Calculator
Ziprasidone hydrochloride monohydrate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1394 mL | 10.6972 mL | 21.3945 mL | 42.789 mL | 53.4862 mL |
| 5 mM | 0.4279 mL | 2.1394 mL | 4.2789 mL | 8.5578 mL | 10.6972 mL |
| 10 mM | 0.2139 mL | 1.0697 mL | 2.1394 mL | 4.2789 mL | 5.3486 mL |
| 50 mM | 0.0428 mL | 0.2139 mL | 0.4279 mL | 0.8558 mL | 1.0697 mL |
| 100 mM | 0.0214 mL | 0.107 mL | 0.2139 mL | 0.4279 mL | 0.5349 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects in preclinical assays predictive of antipsychotic activity. Whereas Ziprasidone is a dopamine antagonist in vitro and in vivo, its most potent action is antagonism of 5-HT2A receptors, where its affinity is an order of magnitude greater than that observed for dopamine D2 sites. Additionally, Ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. Ziprasidone differs from other atypical antipsychotic drugs in several clinically important ways, although further experience is necessary to clarify the significance of these differences.
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Nonisothermal kinetics analysis of the dehydration of ziprasidone hydrochloride monohydrate by thermogravimetry.[Pubmed:24082354]
Indian J Pharm Sci. 2013 May;75(3):361-4.
In the current work the kinetics of dehydration of Ziprasidone hydrochloride monohydrate was studied by nonisothermal thermogravimetry. Ziprasidone hydrochloride monohydrate was heated from 30 to 150 degrees with a heating rate of 5 degrees per min under nitrogen gas atmosphere and weight loss data were collected. Powder X-ray difraction was used to characterize the solid before and after dehydration. The well accepted Coats-Redfern model fitting approach was applied to the thermogravimetry data for the kinetic analysis. Thirteen solid state reaction models were studied; among them one-dimensional diffusion model was found to be the best fit model for this reaction with an excellent correlation 0.9994. The Arrhenius parameters, activation energy, and pre-exponential factor were determined, the values were found to be 28 k.cal/mol and 9.53x10(13) sec(-1), respectively.
Investigation into the effects of the novel antipsychotic ziprasidone on weight gain and reproductive function in female rats.[Pubmed:15863230]
Behav Brain Res. 2005 May 28;160(2):338-43.
Weight gain and sexual dysfunction are serious side effects of certain antipsychotic drugs. Ziprasidone, a novel antipsychotic with a unique receptor binding profile, is reported to have a low propensity for such side effects. Previous results from this laboratory have demonstrated substantial weight gain following sub-chronic treatment with olanzapine and risperidone. Risperidone induced weight gain and markedly impaired reproductive function while olanzapine induced weight gain, without affecting reproductive function. The aim of this study was to investigate effects of ziprasidone on weight gain and reproductive function in female rats. Ziprasidone (1 and 2.5 mg/kg i.p.) or vehicle was administered once daily for 28 days and body weight, food and water intake measured, in addition to histological examination of vaginal lavage to determine the stage of the oestrous cycle. On day 28, the rats were sacrificed and the uterine weights recorded, intra-abdominal fat weight and plasma prolactin levels measured. Ziprasidone failed to induce significant weight gain during weeks 1-3, however, significant weight gain was observed on day 28 at 2.5 mg/kg (p < 0.05). Ziprasidone had no effect on food intake at any time point. A significant reduction in water intake (p < 0.05) was observed during the first week of treatment with 2.5 mg/kg ziprasidone. Ziprasidone had no effect on intra-abdominal fat weight, wet or dry uterine weight or plasma prolactin levels. All ziprasidone treated animals displayed a normal four-day oestrous cycle. This study is the first to report that ziprasidone is without effect on reproductive function or ingestive behaviour in the rat.
Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile.[Pubmed:11513838]
Eur J Pharmacol. 2001 Aug 17;425(3):197-201.
Ziprasidone is a novel antipsychotic agent with a unique combination of pharmacological activities at human receptors. Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone is a 5-HT(1A) receptor agonist and an antagonist at 5-HT(2A), 5-HT(2C) and 5-HT(1B/1D) receptors. Additionally, ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. This unique pharmacological profile of ziprasidone may be related to its clinical effectiveness as a treatment for the positive, negative and affective symptoms of schizophrenia with a low propensity for extrapyramidal side effects, cognitive deficits and weight gain.
Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity.[Pubmed:7562537]
J Pharmacol Exp Ther. 1995 Oct;275(1):101-13.
Ziprasidone (CP-88,059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects in preclinical assays predictive of antipsychotic activity. Whereas the compound is a dopamine antagonist in vitro and in vivo, its most potent action is antagonism of 5-HT2A receptors, where its affinity is an order of magnitude greater than that observed for dopamine D2 sites. Laboratory and clinical findings have led to a hypothesis that antagonism of 5-HT2A receptors in the brain limits the undesirable motor side effects associated with dopamine receptor blockade and improves efficacy against the negative symptoms of schizophrenia. Ziprasidone possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential. The prediction of antipsychotic efficacy without severe motor side effects is supported by the relatively weak potency of ziprasidone to produce catalepsy in animals, contrasted with its potent antagonism of conditioned avoidance responding and dopamine agonist-induced locomotor activation and stereotypy. The compound is well tolerated in animals at doses producing effective dopamine antagonism in the brain. Ziprasidone should be a valuable addition to the treatment of psychotic disorders.
