Asenapine maleate , ≥98%(HPLC) , 85650-56-2

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

CAS NO.：85650-56-2

Empirical Formula: C21H20ClNO5

Molecular Weight: 401.84

MDL number: MFCD00900588

EINECS: 288-064-8

PRODUCT Properties

• Melting point: 141-145°
• Flash point: 9℃
• storage temp.: 2-8°C
• solubility: H2O: ≥10mg/mL
• pka: pK1 <3, pK2 7.52, pK3 8.51(at 25℃)
• form: powder
• color: white to off-white
• Water Solubility: Water : 6.25 mg/mL (15.55 mM; Need ultrasonic and warming)
• InChIKey: GMDCDXMAFMEDAG-CHHFXETESA-N

Description and Uses

Asenapine, a dual antagonist of dopamine D₂and serotonin 5-HT₂receptors, was launched for the acute treatment of schizophreniaand manic or mixed episodes associated with bipolar I disorder in adults. Asenapine exhibits high affinity for serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors (Ki = 2.5, 4.0, 0.06, 0.16, 0.03, 1.6, 0.25, and 0.13 nM, respectively); dopamine D1, D2, D3, and D4 receptors (Ki = 1.4, 0.42, 1.1, and 1.3 nM, respectively); a1- and a2-adrenergic receptors (Ki = 1.2 and 1.2 nM, respectively); and histamine H1 receptors (Ki = 1.0 nM), and moderate affinity for H2 receptors (Ki = 6.2 nM). In in vitro assays, asenapine acts as an antagonist at these receptors. Asenapine has no appreciable affinity for muscarinic cholinergic receptors (e.g., Ki = 8128 nM for M1). Despite its potent binding affinity for multiple receptors, the efficacy of asenapine in schizophrenia is thought to be primarily mediated through a combination of antagonist activity at D2 and 5-HT2A receptors.

Antipsychotic;serotonin 5-HT receptors

Safety

• Symbol(GHS): GHS06,GHS09
• Signal word: Danger
• Hazard statements: H301-H315-H319-H335-H400
• Precautionary statements: P273-P301+P310+P330-P302+P352-P305+P351+P338
• Hazard Codes: Xn,N,T,F
• Risk Statements: 22-36/37/38-50/53-39/23/24/25-23/24/25-11
• Safety Statements: 26-60-61-45-36/37-16
• RIDADR: UN1230 - class 3 - PG 2 - Methanol, solution
• WGK Germany: 3
• HS Code: 29339900