Asenapine

ChemicalBook > CAS DataBase List > Asenapine

Product Name: Asenapine
CAS No.: 65576-45-6
Chemical Name: Asenapine
Synonyms: Saphris;HSDB8061;Asenapine;HSDB 8061;HSDB-8061;Unii-jkz19V908o;Einecs 265-829-4;Asenapine [inn:ban];Asenapine USP/EP/BP;Asenapine free base
CBNumber: CB5879263
Molecular Formula: C17H16ClNO
Formula Weight: 285.772
MOL File: 65576-45-6.mol

Less

Asenapine Property

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)

Less

Safety

Hazardous Substances Data: 65576-45-6(Hazardous Substances Data)

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

Less

N-Bromosuccinimide Price

Cayman Chemical

Product number: 9000496
Product name: (±)-Asenapine
Purity: ≥95%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 9000496
Product name: (±)-Asenapine
Purity: ≥95%
Packaging: 5mg
Price: $93
Updated: 2024/03/01

Cayman Chemical

Product number: 9000496
Product name: (±)-Asenapine
Purity: ≥95%
Packaging: 10mg
Price: $153
Updated: 2024/03/01

TRC

Product number: A788000
Product name: Asenapine
Packaging: 25mg
Price: $435
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FA17998
Product name: Asenapine
Packaging: 10mg
Price: $75
Updated: 2021/12/16

Less

Asenapine Chemical Properties,Usage,Production

Description

(±)-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.

Chemical Properties

Yellow Oil

Uses

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

Definition

ChEBI: (R,R)-asenapine is a 5-chloro-2-methyl-2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole in which both of the stereocentres have R configuration. It is a conjugate base of a (R,R)-asenapine(1+). It is an enantiomer of a (S,S)-asenapine.

Biological Activity

Novel psychopharmacologic agent. Displays antagonist activity at 5-HT, dopamine, noradrenalin and histamine receptor subtypes (pK i values are 8.60, 8.40, 10.15, 9.75, 10.46, 8.84, 9.60, 9.94, 8.85, 8.90, 8.84, 9.38, 8.95, 8.93, 8.9, 9.49, 8.91, 9.00 and 8.21 for 5-HT 1A , 5-HT 1B , 5-HT 2A , 5-HT 2B , 5-HT 2C , 5-HT 5A , 5-HT 6 , 5-HT 7 , D 1 , D 2L , D 2S , D 3 , D 4 , α 1A , α 2A , α 2B , α 2C , H 1 and H 2 receptors respectively). Displays no appreciable affinity for muscarinic receptors. Exhibits potent activity in animal models predictive of antipsychotic efficacy.

Clinical Use

Atypical antipsychotic
Treatment of schizophrenia and bipolar disease

Enzyme inhibitor

This atypical antipsychotic agent (FW = 285.77 g/mol; CAS 65576-45-6), marketed under the trade names Saphris ?, and also known as Org 5222 and (3aRS,12bRS)-rel-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3: 6,7]-oxepino-[4,5-c]pyrrole, is multi-receptor antagonist with the following spectrum of binding interactions: serotonin 5-HT1A receptor, Ki = 2.5 nM; serotonin 5-HT1B receptor, Ki = 4.0 nM; serotonin 5-HT2A receptor, Ki = 0.06 nM; serotonin 5-HT2B receptor, Ki = 0.16 nM; serotonin 5-HT2C receptor, Ki = 0.03 nM; serotonin 5-HT5A receptor, Ki = 1.6 nM; serotonin 5-HT6 receptor, Ki = 1.5 nM; serotonin 5-HT7 receptor, Ki = 0.13 nM; a1- Adrenergic receptor, Ki = 1.2 nM; a2A-Adrenergic receptor, Ki = 1.2 nM; a2B-Adrenergic receptor, Ki = 0.25 nM; a2C-Adrenergic receptor, Ki = 1.2 nM; dopamine D1-receptor, Ki = 1.4 nM; dopamine D2-receptor, Ki = 1.3 nM; dopamine D3-receptor, Ki = 0.4 nM; dopamine D4-receptor, Ki = 1.1 nM; histamine H1-receptor, Ki = 1.0 nM; and histamine H2-receptor, Ki = 6 nM. Like other atypical antipsychotic drugs, asenapine preferentially enhances dopamine and acetylcholine efflux in the rat medial prefrontal cortex and hippocampus. See Reference-x for asenapine’s UV, IR, NMR, and mass spectra as well as X-ray analysis, thermal properties, solubilities and partition coefficient.

Drug interactions

Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids.
Anti-arrhythmics: increased risk of ventricular arrhythmias with anti-arrhythmics that prolong the QT interval; avoid with amiodarone, disopyramide and procainamide (risk of ventricular arrhythmias).
Antidepressants: concentration possibly increased by fluvoxamine; possibly increased paroxetine concentration; concentration of tricyclics possibly increased.
Antiepileptics: antagonises anticonvulsant effect.
Antimalarials: avoid with artemether/lumefantrine.
Antivirals: concentration possibly increased by ritonavir.
Anxiolytics and hypnotics: increased sedative effects.

Metabolism

Metabolism is by direct glucuronidation by UGT1A4 and oxidative metabolism by cytochrome P450 isoenzymes (predominantly CYP1A2) are the primary metabolic pathways for asenapine.
Excretion is 50% renal and 50% via the faeces.

Asenapine Preparation Products And Raw materials

Raw materials

Preparation Products

Less

Asenapine Suppliers

Canada 1 China 116 India 7 The Netherlands 1 United Kingdom 3 United States 17 Global 145

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2923
Advantage: 55

J & K SCIENTIFIC LTD.

Tel: 010-82848833 400-666-7788
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
ProdList: 96815
Advantage: 76

3B Pharmachem (Wuhan) International Co.,Ltd.

Tel: 821-50328103-801 18930552037
Fax: 86-21-50328109
Email: 3bsc@sina.com
Country: China
ProdList: 15848
Advantage: 69

Chembest Research Laboratories Limited

Tel: 021-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6010
Advantage: 61

BeiJing Hwrk Chemicals Limted

Tel: 0757-86329057 18501085097
Fax: 010-89508210
Email: sales3.gd@hwrkchemical.com
Country: China
ProdList: 7639
Advantage: 55

Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070
Fax: +86-25-83453306
Email: info@chemlin.com.cn
Country: China
ProdList: 18088
Advantage: 64

Chemsky（shanghai）International Co.,Ltd.

Tel: 021-50135380
Email: shchemsky@sina.com
Country: China
ProdList: 32344
Advantage: 50

Shanghai Holy Biohemdeviser Co., Ltd

Tel: 021-61551100
Fax: 021-61551100
Country: China
ProdList: 444
Advantage: 57

S.Z. PhyStandard Bio-Tech. Co., Ltd.

Tel: 0755-83725681-603
Fax: +86 755 28094224
Country: China
ProdList: 4505
Advantage: 50

Shanghai T&W Pharmaceutical Co., Ltd.

Tel: +86 21 61551611
Fax: +86 21 50676805
Country: China
ProdList: 9901
Advantage: 58

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7553
Advantage: 61

shanghai cooperpharm co.,LTD .

Tel: +86-021-58975553
Fax: +86-021-58975554
Email: sales@cooperpharm.com
Country: China
ProdList: 1210
Advantage: 56

Bsisun HK Imoprt And Export Company Limited

Tel: +86-18068513926
Fax: 0086-519-85153711
Country: China
ProdList: 1280
Advantage: 55

Nanjing Sunlida Biological Technology Co., Ltd.

Tel: 025-57798810
Fax: 025-57019371
Email: sales@sunlidabio.com
Country: China
ProdList: 3750
Advantage: 55

GIHI CHEMICALS CO.,LTD

Tel: 0086-571-86217390
Fax: 0086-571-86217391
Email: Sales@gihichem.com
Country: China
ProdList: 861
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3423
Advantage: 58

Wuhan DKY Technology Co.,Ltd.

Tel: 27-81302488 18007166089
Fax: 027-81302088
Email: info@dkybpc.com
Country: China
ProdList: 2024
Advantage: 58

Hubei XinyuanShun Chemical Co., Ltd.

Tel: 13971561712, 13995564702, 027-50664929
Fax: 027-50664927
Email: hbeixys2001@163.com
Country: China
ProdList: 3123
Advantage: 55

ChemStrong Scientific Co.,Ltd

Tel: 0755-0755-66853366 13670046396
Fax: 0755-28363542
Email: sales@chem-strong.com
Country: China
ProdList: 17993
Advantage: 56

NINGBO INNO PHARMCHEM CO.,LTD.

Tel: 86-574-27787657
Fax: 86-574-27912196
Email: info@dearchem.com
Country: China
ProdList: 4619
Advantage: 58

Shanghai Xingui Biotechnology Co., Ltd.

Tel: 17501653715
Email: xingui2022@126.com
Country: China
ProdList: 10033
Advantage: 58

Hangzhou J&H Chemical Co., Ltd.

Tel: +86-571-87396432
Fax: 0571-87396431
Email: sales@jhechem.com
Country: China
ProdList: 10015
Advantage: 53

Chizhou Kailong Import and Export Trade Co., Ltd.

Tel
Fax: -
Email: xg01_gj@163.com
Country: China
ProdList: 9503
Advantage: 50

AN PharmaTech Co Ltd

Tel: 86(21)68097365
Fax: 86(21)33321566
Email: sales@anpharma.net
Country: China
ProdList: 4901
Advantage: 55

SPIRO PHARMA

Tel
Fax: -
Email: eric_feng1954@126.com
Country: China
ProdList: 9254
Advantage: 55

Pharmacodia (Beijing) Co.,Ltd

Tel: +86-400-851-9921
Fax: +86-10-82826195
Email: sales@pharmacodia.com
Country: China
ProdList: 2317
Advantage: 55

parabiochem

Tel: 025-83453382-8005
Fax: 025-83453382
Email: sale@parabiochem.com
Country: China
ProdList: 9604
Advantage: 55

Shijiazhuang XinZhaoYang Chemical Technology Co., Ltd.

Tel: 0311-69032540 13931172911
Fax: 0311-69032540
Email: 2636239065@qq.com
Country: China
ProdList: 290
Advantage: 55

Raw material medicin reagent co.,Ltd

Tel
Email: sales@njromanme.com
Country: China
ProdList: 4534
Advantage: 58

Chengdu Dianchun Technology Co., Ltd

Tel: 400-1166-196 18502815961
Fax: QQ：800101999
Email: cdhxsj@163.com
Country: China
ProdList: 14623
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 17754423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8011
Advantage: 62

Beijing Solarbio Science & Tecnology Co., Ltd.

Tel: 010-50973130 4009686088
Email: 3193328036@qq.com
Country: China
ProdList: 29796
Advantage: 68

Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131981
Advantage: 58

Henan Anky Chemical Technology Co., Ltd.

Tel: 17836913271
Fax: 0374-8348899
Email: 3224305243@qq.com
Country: China
ProdList: 2790
Advantage: 58

Amatek Scientific Co. Ltd.

Tel: 0512-56316828
Fax: 0512-56316826
Email: info@amateksci.com
Country: China
ProdList: 28821
Advantage: 58

Zhongshan Resi Biotechnology Co., Ltd.

Tel: 13715524166 13326948089
Fax: +86 760 8866 5202
Email: resicn@resicn.com
Country: China
ProdList: 520
Advantage: 58

Aikon International Limited

Tel: 025-58859352 18068836627
Fax: 02557626880
Email: sales01@aikonchem.com
Country: China
ProdList: 15085
Advantage: 58

Alchemist-pharm chemical Technology Co. Ltd.

Tel: 0371-67991738 13783628208
Fax: QQ 412703949
Email: carl@alchemist-pharm.com
Country: China
ProdList: 1877
Advantage: 58

Hubei Xinyuanshun Pharmaceutical Chemical Co., Ltd.

Tel: 027-51831887 15337167856
Fax: 027-51837635 QQ1165326703
Email: hubeixinyuanshun@163.com
Country: China
ProdList: 10305
Advantage: 58

Nanjing the parson's chemical technology co., LTD

Tel: 025-58786926 18951781718
Fax: 025-58786926
Email: zbbgz2009@163.com
Country: China
ProdList: 311
Advantage: 58

Shanghai Jizhi Biochemical Technology Co. Ltd.

Tel: 400-400-400-9004166 18616739031
Email: 3007523370@qq.com
Country: China
ProdList: 52712
Advantage: 58

Shenzhen Polymeri Biochemical Technology Co., Ltd.

Tel: +86-400-002-6226 13028896684
Email: sales@rrkchem.com
Country: China
ProdList: 55936
Advantage: 58

Hefei TNJ Chemical Industry Co.,Ltd.

Tel: 0551-65418684 +8618949823763
Fax: 0086-551-65418684
Email: sales@tnjchem.com
Country: China
ProdList: 25363
Advantage: 58

Wuhan Golt Biotech Co., Ltd.

Tel: +8615389281203
Email: maria@goltbiotech.com
Country: China
ProdList: 980
Advantage: 58

Dideu Industries Group Limited

Tel: +86-29-89586680 +86-15129568250
Email: 1026@dideu.com
Country: China
ProdList: 28098
Advantage: 58

Baoji Guokang Bio-Technology Co., Ltd.

Tel: 0917-3909592 13892490616
Fax: 09173909592
Email: gksales1@gk-bio.com
Country: China
ProdList: 9331
Advantage: 58

Jinan Ruisi Pharmaceutical Technology Co., LTD

Tel: 0531-69900633 18340090523
Email: changyuan20@163.com
Country: China
ProdList: 1833
Advantage: 58

Chemwill Asia Co.,Ltd.

Tel: 86-21-51086038
Fax: 86-21-51861608
Email: chemwill_asia@126.com
Country: CHINA
ProdList: 23931
Advantage: 58

DC Chemicals

Tel: 021-58447131 13564518121
Email: sales@dcchemicals.com
Country: China
ProdList: 9414
Advantage: 58

Tianjin shijia biomedical technology co., LTD

Tel: 15022261580;411316762
Email: tjshj1212@163.com
Country: China
ProdList: 2347
Advantage: 58

Less

View Lastest Price from Asenapine manufacturers

Dideu Industries Group Limited

Product: Asenapine 65576-45-6
Price: US $1.10/g
Min. Order: 1g
Purity: 99.9%
Supply Ability: 100 Tons min
Release date: 2021-07-26

Zhuozhou Wenxi import and Export Co., Ltd

Product: Asenapine 65576-45-6
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 65576-45-6
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-08

65576-45-6, AsenapineRelated Search:

Asenapine Maleate Asenapine related impurities N-DesMethyl Asenapine-d4 5-Chloro-2-methyl-2,3-dihydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole-(2H)-one Asenapine-N-beta-D-glucuronide Paricalcitol ILOPERIDONE SGWOPWVMYXQVHJ-UHFFFAOYSA-N Reaxys ID: 3623864 (3aR,12bR)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one (3aS,12bS)-2-Methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole Entacapone 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 impurity A Asenapine (R)-3-PHENYL-PYRROLIDINE HYDROCHLORIDE

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

Asenapine

(3aR,12bR)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole

ORG 5222;ORG-5222;ORG5222

1H-Dibenz(2,3:6,7)oxepino(4,5-C)pyrrole, 5-chloro-2,3,3A,12B-tetrahydro-2-methyl-, (3ar,12br)-rel-

1H-Dibenz(2,3:6,7)oxepino(4,5-C)pyrrole, 5-chloro-2,3,3A,12B-tetrahydro-2-methyl-, trans-

Asenapine [inn:ban]

Einecs 265-829-4

Unii-jkz19V908o

(3aR*,12bR*)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrolemaleate

(3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole

(3aS,12bS)-5-chloro-2-Methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole Maleate

Saphris

Asenapine, racemic mixture

Asenapine USP/EP/BP

trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:...

Asenapine Impurity 2

Asenapine free base

HSDB 8061

HSDB8061

HSDB-8061

Asenapine (Org 5222)

65576-45-6

C17H16CINOC4H4O4

Aromatics

Heterocycles

Intermediates & Fine Chemicals

Pharmaceuticals