Asenapine maleate

SKU: orb1223845

Description

Asenapine maleate (Org 5222) is a potent psychopharmacologic agent that shows high affinity for 5-HT, dopamine, histamine and adrenoceptors; shows much lower affinity (pKi<5) for muscarinic receptor; behaves as a potent antagonist 5-HT receptors (5-HT2A pKB=9.0), dopaime and adrenoceptors; shows strong antipsychotic potential in vivo.Schizophrenia Approved(In Vitro):Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors.(In Vivo):Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.

Key Properties

• CAS Number: 85650-56-2
• MW: 401.8402
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀ClNO₅
• SMILES: CN1C[C@H]2[C@H](C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O
• Target: Adrenergic Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.
• In Vitro:
  Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Org 5222 maleate | Org-5222 maleate | Org5222 maleate

Quick Database Links

Gene Symbol

Adrenergic Receptor