A7861

Asenapine maleate

≥98% (HPLC)

• Synonym(s): (3aRS,12bRS)-5-Chloro-2-methyl-2,3,3a,12btetrahydro-1Hdibenzo[2,3:6,7]oxepino[4,5-c]pyrrole (2Z)-2-butenedioate, Org 5222, trans-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole maleate
• Empirical Formula (Hill Notation): C₁₇H₁₆ClNO ·C₄H₄O₄
• CAS Number: 85650-56-2
• Molecular Weight: 401.84
• EC Number: 288-064-8
• UNSPSC Code: 12352200
• PubChem Substance ID: 329770943
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: powder
• color: white to off-white
• solubility: H₂O: ≥10 mg/mL
• originator: Merck & Co., Inc., Kenilworth, NJ, U.S.
• storage temp.: 2-8°C
• SMILES string: OC(=O)\C=C/C(O)=O.CN1C[C@H]2[C@H](C1)c3cc(Cl)ccc3Oc4ccccc24
• InChI: 1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,15-;/m1./s1
• InChI key: GMDCDXMAFMEDAG-CHHFXETESA-N

Description

General description

Asenapine maleate acts as an antimanic. It belongs to the family of dibenzoxepinopyrrolidines. Asenapine is considered to be a weak inhibitor of cytochrome P450 2D6 (CYP2D6). It increases the level of dopamine, norepinephrine and acetylcholine in brain.

Application

Asenapine maleate has been used as a stressor in studying the Fos expression in forebrain structures of rat models.

Asenapine maleate is a serotonin 5-HT and dopamine D2 receptor antagonist. Asenapine maleate can be used to treat schizophrenia and bipolar mania.

Biochem/physiol Actions

Asenapine maleate is a 5-HT receptor antagonist (5-HT_1A,_1B, 5-HT_{2A, 2B, 2C}, 5-HT_5A, 5-HT₆ and 5-HT₇), a D2 antagonist, and an antipsychotic.

Features and Benefits

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Safety Information

• Pictograms: GHS06,GHS09
• Signal Word: Danger
• Hazard Statements: H301,H315,H319,H335,H400
• Precautionary Statements: P273 - P301 + P310 + P330 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Acute Tox. 3 Oral - Aquatic Acute 1 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Target Organs: Respiratory system
• Storage Class Code: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable