Asenapine , 96% , 65576-45-6

CAS NO.：65576-45-6

Empirical Formula: C17H16ClNO

Molecular Weight: 285.772

MDL number: MFCD09838016

EINECS: 2658294

PRODUCT Properties

• Boiling point: 357.9±42.0 °C(Predicted)
• Density: 1.231
• storage temp.: Store at +4°C
• solubility: DMSO:50.0(Max Conc. mg/mL);174.97(Max Conc. mM)
• form: A solid
• pka: 9.50±0.20(Predicted)
• color: White to off-white

Description and Uses

(±)-Asenapine is an atypical antipsychotic. It binds to dopamine D_1-4, α-adrenergic, and histamine receptors (K_is = 0.42-1.45, 0.32-1.26, and 1-6.17 nM, respectively), as well as the serotonin (5-HT) receptor subtypes 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2B, 5-HT_2C, 5-HT_5A, 5-HT₆, and 5-HT₇ (K_is = 0.03-3.98 nM). (±)-Asenapine inhibits the suppression of neuron firing induced by the 5-HT_2A, dopamine D₂, and α₂-adrenergic receptor agonists 2,5-dimethoxy-4-iodoamphetamine (DOI), apomorphine, and clonidine , respectively, in rat brain (ED₅₀s = 75, 40, and 85 μg/kg, respectively). In vivo, (±)-asenapine (0.05-0.2 mg/kg, s.c.) increases extracellular dopamine levels in the medial prefrontal cortex (mPFC), nucleus accumbens (NAc), and lateral striatum and suppresses the conditioned avoidance response in rats. It prevents acute and chronic phencyclidine-induced deficits in cued reversal learning in rats when administered at a dose of 0.075 mg/kg. Formulations containing asenapine have been used in the treatment of schizophrenia and bipolar I disorder.

Combined serotonin (5HT2) and dopamine (D2) receptor antagonist; structurally related to Mianserin. Antipsychotic

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H319-H315-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P