| Name | Ziprasidone |
| Description | Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity. |
| In vitro | Ziprasidone demonstrates the ability to inhibit the significant increase in food intake induced by olanzapine in rats, indicating an intrinsic protective mechanism against drug-induced hyperphagia. Furthermore, Ziprasidone significantly enhances the immunoreactivity of NGF and ChAT in the dentate gyrus, CA1, and CA3 regions of the rat hippocampus. In anesthetized rats, Ziprasidone exhibits a dose-dependent reduction in the activity of midline thalamic neurons, similar to atypical antipsychotic drugs such as clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.), with an ED50 value of 300 mg/kg i.v. Additionally, Ziprasidone has a relatively low blocking effect on the wild-type hERG current in Xenopus oocytes, with an IC50 of 2.8 mM. |
| In vivo | Ziprasidone selectively blocks wild-type hERG currents in stably transfected HEK-293 cells in a voltage and concentration-dependent manner with an IC(50) of 120nM. It demonstrates minimal torsadogenic risk as evidenced by minimal hERG current blockade during depolarized voltages (-20 or +30mV) or assessed via envelope of tails experiments at +30mV. Ziprasidone significantly prolongs the deactivation time constant of hERG currents at -50mV. It acts as a 5-HT(1A) receptor agonist and antagonizes 5-HT(2A), 5-HT(2C), and 5-HT(1B/1D) receptors. The compound's potency in inhibiting neuronal uptake of 5-HT and norepinephrine is similar to that of the antidepressant imipramine. Ziprasidone also exhibits high affinity for human 5-HT receptors and human dopamine D(2) receptors. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 13.5 mg/mL (32.69 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.42 mM), Sonication is recommended.
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| Keywords | α2A-adrenergic receptor | α1A-adrenergic receptor | Ziprasidone | Serotonin Receptor | serotonin | norepinephrine transporter (NET) | Inhibitor | inhibit | HistamineReceptor | Histamine Receptor | HEK-293 | H1 receptor | DopamineReceptor | Dopamine Receptor | Dopamine | D3 | D2 | D1 | CP88059 | CP 88059 | antipsychotic agent | AdrenergicReceptor | Adrenergic Receptor | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT7 | 5-HT6 | 5-HT2C | 5-HT2A | 5-HT1D | 5-HT1B | 5-HT1A | 5-HT transporter | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Meclizine dihydrochloride | Dapoxetine hydrochloride | Lidocaine | Famotidine | Octopamine hydrochloride | Sodium butanoate | D-Menthol | Oxolinic acid | Alginic acid | Trazodone hydrochloride | Mianserin hydrochloride |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
