Ziprasidone hydrochloride

SKU: orb1311003

Description

Ziprasidone hydrochloride

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 122883-93-6
• MW: 449.4
• Purity: 99.82%
• Formula: C₂₁H₂₂CL₂N₄OS
• SMILES: Clc1c(cc2CC(=O)Nc2c1)CCN1CCN(c2nsc3ccccc23)CC1.Cl
• Target: Norepinephrine,Histamine Receptor,Adrenergic Receptor,5-HT Receptor,Dopamine Receptor
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (7.34 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:83 mg/mL (184.69 mM)

Bioactivity

• Target IC50:
  5-HT1A receptor (rat):3.4 nM (Ki)|5-HT2A:0.42 nM (Ki)|5-HT1A receptor (human):2.5 nM (Ki)|D2 receptor (rat):4.8 nM (Ki)
• In Vivo:
  Ziprasidone blocks wild-type hERG currents in a voltage and concentration-dependent manner with an IC(50) of 120 nM in stably transfected HEK-293 cells. Minimal hERG current blockade by ziprasidone is estimated during depolarized voltages (-20 or +30 mV) or assessed via envelope of tail test (+30 mV). The compound significantly prolongs the time constant of the slow component of hERG current deactivation at -50 mV. Ziprasidone acts as a 5-HT(1A) receptor agonist and antagonizes 5-HT(2A), 5-HT(2C), and 5-HT(1B/1D) receptors, similar to the antidepressant imipramine in inhibiting serotonin and norepinephrine neuronal uptake. It also exhibits high affinity for human 5-HT receptors and dopamine D(2) receptors.
• In Vitro:
  Ziprasidone exhibits an inherent protective mechanism against drug-induced increases in food intake, demonstrated by its ability to inhibit the significant enhancement of food consumption caused by olanzapine in rats. It also induces a notable upregulation of NGF and ChAT immunoreactivity in the hippocampal regions dentate gyrus, CA1, and CA3 of rats. Furthermore, Ziprasidone dose-dependently decreases the activity of midbrain central tegmental field neurons (ED50 = 300 mg/kg i.v.), similar to atypical antipsychotics like clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.) in anesthetized rats. In Xenopus oocytes, Ziprasidone displays a lower inhibitory effect (IC50 = 2.8 mM) on the wild-type hERG current.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

H1 receptor, HistamineReceptor, Histamine Receptor, neuronal, norepinephrine transporter (NET), CP 88059, CP 88059 Hydrochloride, CP88059, CP88059 Hydrochloride, CP-88059 hydrochloride, D3, D2, D1, Dopamine Receptor, Dopamine, DopamineReceptor, 5-HT7, 5HTReceptor, 5-HT6, AdrenergicReceptor, Adrenergic Receptor, 5HT Receptor, 5-HT Receptor, 5-HT1B, 5-HT1D, 5-HT1A, 5-HT transporter, 5-HT2C, 5-HT2A, antipsychotic, Ziprasidone, Ziprasidone HCl, rats, Sprague-Dawley, uptake, α1A-adrenergic receptor, α2A-adrenergic receptor

Compound Identifiers

PubChem CID

219099