Asenapine maleate

Research use only, not for human use.

Asenapine maleate (Org 5222) is a potent psychopharmacologic agent that shows high affinity for 5-HT, dopamine, histamine and adrenoceptors.

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.

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.

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.

Org 5222 maleate | Org-5222 maleate | Org5222 maleate

GPCR/G Protein

Adrenergic Receptor

5-HT2A|5-HT2B|5-HT2C|5-HT6|5-HT7

Neurological Disease

Schizophrenia

85650-56-2

401.8402

C21H20ClNO5

>98% (HPLC)

10 mM in DMSO

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

1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, (3aR,12bR)-rel-, (2Z)-2-butenedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years