Asenapine Maleate
- Product Name
- Asenapine Maleate
- CAS No.
- 85650-56-2
- Chemical Name
- Asenapine Maleate
- Synonyms
- Org 5222;NSC62790;NSC 62790;NSC-62790;Asenne maleate;Unii-cu9463U2E2;Org5222 Maleate;Saphris Maleate;Org-5222 Maleate;Org 5222 Maleate
- CBNumber
- CB2932538
- Molecular Formula
- C21H20ClNO5
- Formula Weight
- 401.84
- MOL File
- 85650-56-2.mol
Asenapine Maleate Property
- 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
Safety
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
H400Very toxic to aquatic life
- Precautionary statements
-
P273Avoid release to the environment.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- A7861
- Product name
- Asenapine maleate
- Purity
- ≥98% (HPLC)
- Packaging
- 10mg
- Price
- $82.1
- Updated
- 2024/03/01
- Product number
- A7861
- Product name
- Asenapine maleate
- Purity
- ≥98% (HPLC)
- Packaging
- 50mg
- Price
- $326
- Updated
- 2024/03/01
- Product number
- 3737
- Product name
- Asenapine maleate
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $588
- Updated
- 2021/12/16
- Product number
- 3737
- Product name
- Asenapine maleate
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $136
- Updated
- 2021/12/16
- Product number
- A788025
- Product name
- Asenapine maleate
- Packaging
- 100mg
- Price
- $120
- Updated
- 2021/12/16
Asenapine Maleate Chemical Properties,Usage,Production
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 has been used as a stressor in studying the Fos expression in forebrain structures of rat models.
Uses
Asenapine Maleate is a 5-HT receptor antagonist developed for the treatment of acute schizophrenia and bipolar mania.
Definition
ChEBI: (S,S)-asenapine maleate is a maleate salt obtained by combining equimolar amounts of (S,S)-asenapine and maleic acid. It contains a (S,S)-asenapine(1+). It is an enantiomer of a (R,R)-asenapine maleate.
brand name
Saphris
General Description
Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder. The drug is marketed under the trade names Saphris? and Sycrest. This certified solution standard is suitable for LC/MS or GC/MS applications in clinical toxicology, forensic testing, or pharmaceutical research.
Biochem/physiol Actions
Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.
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.
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.
storage
Store at +4°C
Asenapine Maleate Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Asenapine Maleate manufacturers
- Product
- Asenapine Maleate 85650-56-2
- Price
- US $0.00/Kg/Bag
- Min. Order
- 10g
- Purity
- 99.5%min HPLC
- Supply Ability
- 10KGS
- Release date
- 2021-07-07
- Product
- Asenapine Maleate 85650-56-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10
- Product
- Asenapine Maleate 85650-56-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-09