Cariprazine hydrochloride

SKU: orb1298981

Description

Cariprazine hydrochloride

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1083076-69-0
• MW: 463.87
• Purity: 100.00%
• Formula: C₂₁H₃₃Cl₃N₄O
• SMILES: Cl.CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCN(CC2)c2cccc(Cl)c2Cl)CC1
• Target: Dopamine Receptor,5-HT Receptor
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);H2O:1.64 mg/mL (3.54 mM)

Bioactivity

• Target IC50:
  D3 receptor:0.085 nM (Ki) |5-HT1A receptor:2.6 nM (Ki)|D2 receptor:0.49 nM (Ki)
• In Vivo:
  Cariprazine occupied D(2)/D(3) receptors in a dose-dependent and saturable manner, with the lowest dose occupying ~5% of receptors and the highest dose showing more than 90% occupancy. 5-HT(1A) receptor occupancy was considerably lower compared with D(2)/D(3) occupancy at the same doses, with a maximal value of ~30% for the raphe nuclei.
• Animal Research:
  Three monkeys using the following PET radioligands: [(11)C]MNPA (an agonist at D(2) and D(3) receptors), [(11)C]raclopride (an antagonist at D(2) and D(3) receptors), and [(11)C]WAY-100635 (an antagonist at 5-HT(1A) receptors). During each experimental day, the first PET measurement was a baseline study, the second after a low dose of cariprazine, and the third after the administration of a high dose.

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

RGH 188, RGH 188 Hydrochloride, RGH188, RGH-188, RGH188 hydrochloride, RGH188 Hydrochloride, RGH-188 Hydrochloride, Serotonin Receptor, D3, D2, DopamineReceptor, Dopamine Receptor, Dopamine, 5HT Receptor, 5-HT Receptor, 5HTReceptor, 5-hydroxytryptamine Receptor, Cariprazine, Cariprazine HCl, Cariprazine Hydrochloride, Cariprazine hydrochloride, Inhibitor, inhibit

Compound Identifiers

PubChem CID

25096873