Asenapine Maleate

ChemicalBook > CAS DataBase List > 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

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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

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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

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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.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: A7861
Product name: Asenapine maleate
Purity: ≥98% (HPLC)
Packaging: 10mg
Price: $82.1
Updated: 2024/03/01

Sigma-Aldrich

Product number: A7861
Product name: Asenapine maleate
Purity: ≥98% (HPLC)
Packaging: 50mg
Price: $326
Updated: 2024/03/01

Tocris

Product number: 3737
Product name: Asenapine maleate
Purity: ≥98%(HPLC)
Packaging: 50
Price: $588
Updated: 2021/12/16

Tocris

Product number: 3737
Product name: Asenapine maleate
Purity: ≥98%(HPLC)
Packaging: 10
Price: $136
Updated: 2021/12/16

TRC

Product number: A788025
Product name: Asenapine maleate
Packaging: 100mg
Price: $120
Updated: 2021/12/16

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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

WUHAN FORTUNA CHEMICAL CO., LTD

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

Zhuozhou Wenxi import and Export Co., Ltd

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

Zhuozhou Wenxi import and Export Co., Ltd

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

85650-56-2, Asenapine MaleateRelated Search:

trans-(+/-)-11-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one Carbon tetrachloride Maleic acid Asenapine N-Oxide 1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one, 11-chloro-2,3,3a,12b-tetrahydro-2-Methyl-, (3aR,12bS)-rel- Saphris hydrochloride Asenapine N-DesMethyl Asenapine-d4 5-Chloro-2-methyl-2,3-dihydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole-(2H)-one Asenapine 13C D3 HCl Asenapine-N-Glucuronide (Mixture of Diastereomers) Deschloro Asenapine (S,S)-Asenapine Maleate Asenapine 11-Hydroxysulfate Cis-Asenapine N-Desmethyl Asenapine Hydrochloride (3aR,12bR)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepin[4,5-c]pyrrole maleate Asenapine impurity A

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

1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, trans-, (Z)-2-butenedioate (1:1)

Org 5222 Maleate

Org5222 Maleate

Org-5222 Maleate

Saphris Maleate

H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, (3aS,12bS)-

Asenapine maleate solution

(3aRS,12bRS)-5-Chloro-2-methyl-2,3,3a,12btetrahydro-1Hdibenzo[2,3:6,7]oxepino[4,5-c]pyrrole (2Z)-2-butenedioate

Asenapine maleate, 98%, a 5-HT receptor antagonist

SAPHRIS MALEATE; ORG 5222 MALEATE; ORG-5222 MALEATE; ORG5222 MALEATE

Asenapine maleate, racemic mixture

Asenapine Maleate USP/EP/BP

Asenne maleate

trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole maleate

Asenapine maleate (Org 5222 maleate)

Asenapine maleateQ: What is Asenapine maleate Q: What is the CAS Number of Asenapine maleate Q: What is the storage condition of Asenapine maleate Q: What are the applications of Asenapine maleate

NSC 62790

NSC62790

NSC-62790

Azenapine maleate

Asenapine maleate salt, racemic mixture

rel-Asenapine maleate

Acenapine maleate

Org 5222 maleate|||Org 5222

85650-56-2

C17H16ClNOC4H4O4

Inhibitors

Saphris

API