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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Neuronal Signaling>5-HT Receptor modulators>Asenapine Maleate
Asenapine Maleate
  • Asenapine Maleate

Asenapine Maleate

Price $7
Package 1KG
Min. Order: 1KG
Update Time: 2019-09-02

Product Details

Product Name: Asenapine Maleate CAS No.: 85650-56-2
Min. Order: 1KG Purity: 99%
Supply Ability: JD 486 Release date: 2019/09/02
Product Name:
Asenapine Maleate
Synonyms:
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole maleate;Org 5222;Asenapine maleate;Einecs 288-064-8;Unii-cu9463U2E2;Org 5222 Maleate;Org5222 Maleate;Org-5222 Maleate
CAS:
85650-56-2
MF:
C21H20ClNO5
MW:
401.8402
EINECS:
288-064-8
Product Categories:
Saphris;Inhibitors;-
Mol File:
85650-56-2.mol
Article illustration
 
Asenapine Maleate Chemical Properties
Melting point 
141-145°
Fp 
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
InChIKey
GMDCDXMAFMEDAG-CHHFXETESA-N
 
Safety Information
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
MSDS Information
 
 
Asenapine Maleate Usage And Synthesis
Description
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.
Chemical Properties
White Solid
Originator
Organon (US)
Uses
Antipsychotic;serotonin 5-HT receptors
Uses
Asenapine Maleate is a 5-HT receptor antagonist developed for the treatment of acute schizophrenia and bipolar mania.
Brand name
Saphris
Side effects
The most common adverse effects associated with asenapine treatment include insomnia, somnolence, nausea, anxiety, agitation, headache, vomiting, constipation, and psychosis. In placebo-controlled trials with risperidone, aripiprazole, and olanzapine in elderly subjects with dementia, there was a higher incidence of cerebrovascular adverse reactions (cerebrovascular accidents and transient ischemic attacks) including fatalities compared to placebo-treated subjects. Asenapine is not approved for the treatment of patients with dementia-related psychosis.
Chemical Synthesis
The chemical synthesis of asenapine can be achieved by several different methods. A concise synthesis of asenapine begins with the Horner-Emmons condensation of diethyl (5-chloro-2-fluoro)benzyl phosphonate with salicylaldehyde to produce the corresponding stilbene derivative, which undergoes a 1,3-dipolar cycloaddition reaction with trimethylamine-N-oxide in the presence of lithium diisopropylamide to furnish a trans-3,4-diarylpyrrolidine intermediate. Then, a base-catalyzed intramolecular cyclization involving the nucleophilic displacement of the fluoro group by the phenolic hydroxyl group affords asenapine, which is finally treated with maleic acid in ethanol to yield the corresponding maleate salt.

Company Profile Introduction

Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals. Mainly deals in the sales of: Pharmaceutical intermediates OLED intermediates: Pharmaceutical intermediates; OLED intermediates;

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