Ziprasidone

SKU: orb1311002

Description

Ziprasidone (Geodon) is a combined serotonin and dopamine receptor antagonist with potent antipsychotic activity. It is widely used in neuroscience research to study schizophrenia mechanisms and evaluate pharmacological effects in both cellular and animal models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 146939-27-7
• MW: 412.94
• Purity: 99.53% (May vary between batches)
• Formula: C₂₁H₂₁ClN₄OS
• SMILES: C(CC=1C=C2C(=CC1Cl)NC(=O)C2)N3CCN(C=4C=5C(SN4)=CC=CC5)CC3
• Target: Histamine Receptor|||5-HT Receptor|||Adrenergic Receptor|||Dopamine Receptor|||Norepinephrine
• Solubility: DMSO:13.5 mg/mL (32.69 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.42 mM)

Bioactivity

• Target IC50:
  5-HT1A receptor (human):2.5 nM (Ki)|5-HT2A:0.42 nM (Ki)|5-HT1A receptor (rat):3.4 nM (Ki)|D2 receptor (rat):4.8 nM (Ki)
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Zeldox, Ziprasidone, serotonin, Serotonin Receptor, α2A-adrenergic receptor, α1A-adrenergic receptor, CP 88059, DopamineReceptor, Dopamine Receptor, Dopamine, CP-88059, CP88059, D1, D3, D2, Adrenergic Receptor, AdrenergicReceptor, 5HT Receptor, 5-HT2A, 5-HT2C, 5-HT transporter, 5-HT Receptor, 5-HT1D, 5-HT1B, 5-HT1A, 5-hydroxytryptamine Receptor, 5HTReceptor, 5-HT7, 5-HT6, antipsychotic agent, H1 receptor, Geodon, Inhibitor, Histamine Receptor, HistamineReceptor, HEK-293, norepinephrine transporter (NET), inhibit

Compound Identifiers

PubChem CID

60854