Rat 5-HT_2A ( Ki = 0.42 nM ); Rat 5-HT_1A Receptor ( Ki = 3.4 nM ); Rat D₂ Receptor ( Ki = 4.8 nM )

Ziprasidone hydrochloride monohydrate (0-500 nM, 150 seconds) blocks wild-type hERG currents [2]. Cell Viability Assay[2] Cell Line: HEK-293 Cell Concentration: 0-500 nM Incubation Time: 150 sec Results: Blocks wild-type hERG current (IC50 = 120 nm) in a voltage- and concentration-dependent manner.

Ziprasidone hydrochloride monohydrate (oral gavage; 20 mg/kg; once daily; 7 weeks) results in weight loss, lower physical activity levels, higher resting energy expenditure, and increased thermogenesis in the cold [3] . Animal model: 8-week-old female Sprague-Dawley rats, weighing 200 to 250 g[3] Dosage: 20 mg/kg Administration method: oral gavage; 20 mg/kg; once a day; 7-week results: significant weight loss (P = 0.031), had lower levels of physical activity (P = 0.016), had higher resting energy expenditure (P < 0.001), and showed greater thermogenic capacity when cold (P < 0.001).

Use of Ziprasidone During Pregnancy and Lactation ◉ Overview of Use During Lactation
Due to limited published experience regarding the use of ziprasidone during lactation, alternative antipsychotic medications may be preferred, especially when breastfeeding newborns or premature infants. A safety rating system indicates that ziprasidone can be used with caution during lactation. Infants breastfed by mothers taking ziprasidone should be monitored for excessive sedation, irritability, feeding difficulties, and extrapyramidal symptoms such as tremors and abnormal muscle movements.
◉ Effects on Breastfed Infants
A woman took ziprasidone 40 mg and citalopram 60 mg daily throughout her pregnancy and postpartum. She breastfed extensively and occasionally had formula fed by another person. At 6 months of age, a pediatric examination found the infant to be in good health and growing normally.
A comparison was made between breastfeeding patients taking second-generation antipsychotics (n = 576) registered with the National Atypical Antipsychotic Pregnancy Registry and a breastfeeding control group (n = 818) not taking second-generation antipsychotics. Among patients taking second-generation antipsychotics, 60.4% were taking more than one psychotropic medication. A review of pediatric medical records showed no adverse reactions in infants, regardless of whether they received monotherapy or combination therapy with second-generation antipsychotics. No cases of women taking ziprasidone were reported.
◉ Effects on Lactation and Breast Milk
Elevated prolactin levels and galactorrhea have been reported during ziprasidone treatment, commonly in adolescents. However, compared to phenothiazines, the increase in prolactin is likely to be more transient and milder. For mothers who have established lactation, prolactin levels may not affect their ability to breastfeed.
A comparison was made between breastfeeding patients taking second-generation antipsychotics (n = 576) registered with the National Registry for Atypical Antipsychotic Pregnancy and a control group of breastfeeding patients with a primary diagnosis of major depressive disorder and anxiety (n = 818). The control group typically received selective serotonin reuptake inhibitors (SSRIs) or selective serotonin and norepinephrine reuptake inhibitors (SNRIs) but did not use second-generation antipsychotics. Among women taking second-generation antipsychotics, 60.4% were taking more than one psychotropic medication concurrently, compared to 24.4% in the control group. Among women taking second-generation antipsychotics, 59.3% reported breastfeeding, compared to 88.2% in the control group. At 3 months postpartum, the exclusive breastfeeding rate was 23% among women taking second-generation antipsychotics, compared to 47% in the control group. The number of women taking ziprasidone was not reported.

[1]. 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry. 2000;48(3):229-237.

[2]. Block of hERG channel by ziprasidone: biophysical properties and molecular determinants. Biochem Pharmacol. 2006 Jan 12;71(3):278-86.

[3]. The effect of ziprasidone on body weight and energy expenditure in female rats. Metabolism. 2012 Jun;61(6):787-93.

See also: Ziprasidone Hydrochloride (Note moved to).

C21H24CL2N4O2S

467.409

466.099

C, 53.96; H, 5.18; Cl, 15.17; N, 11.99; O, 6.85; S, 6.86

138982-67-9

Ziprasidone; 146939-27-7; Ziprasidone-d8; 1126745-58-1; Ziprasidone hydrochloride;122883-93-6; Ziprasidone mesylate trihydrate; 199191-69-0

60853

Pink to red solid powder

554.8ºC at 760 mmHg

300°C

2.38E-12mmHg at 25°C

4.687

3

6

4

30

573

0

ClC1C([H])=C2C(C([H])([H])C(N2[H])=O)=C([H])C=1C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])N(C2C3=C([H])C([H])=C([H])C([H])=C3SN=2)C([H])([H])C1([H])[H]

ZCBZSCBNOOIHFP-UHFFFAOYSA-N

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

5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one;hydrate;hydrochloride

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

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: ~25 mg/mL (~53.5 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: 2.5 mg/mL (5.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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 (Please use freshly prepared in vivo formulations for optimal results.)