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Asenapine

Asenapine Structure
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
Molecular Weight:
285.772
MOL File:
65576-45-6.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:12
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Asenapine 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

SAFETY

Risk and Safety Statements

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
NFPA 704
0
2 0

Asenapine Chemical Properties,Uses,Production

Description

(±)-Asenapine is an atypical antipsychotic. It binds to dopamine D1-4, α-adrenergic, and histamine receptors (Kis = 0.42-1.45, 0.32-1.26, and 1-6.17 nM, respectively), as well as the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and 5-HT7 (Kis = 0.03-3.98 nM). (±)-Asenapine inhibits the suppression of neuron firing induced by the 5-HT2A, 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

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.

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.

Asenapine Preparation Products And Raw materials

Raw materials

Asenapine Maleate trans-(+/-)-11-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 2-Chlorophenylacetic acid

Preparation Products

Asenapine Suppliers

Global( 144)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
VGS SYNTHESIS PRIVATE LIMITED +91-9866975588 +91-9866975588 Hyderabad, India 1818 58 Inquiry
Ebenezer Industries Gujarat, India 96 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
Chiral Biosciences Limited 09441920381 Mallapur, India 41 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Pharma Affiliates 172-5066494 Haryana, India 6761 58 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29898 58 Inquiry
Chongqing Chemdad Co., Ltd +86-023-6139-8061 +86-86-13650506873 China 39916 58 Inquiry
Supplier Advantage
VGS SYNTHESIS PRIVATE LIMITED 58
Ebenezer Industries 58
SynZeal Research Pvt Ltd 58
Pharmaffiliates Analytics and Synthetics P. Ltd 58
Chiral Biosciences Limited 58
CLEARSYNTH LABS LTD. 58
Pharma Affiliates 58
ATK CHEMICAL COMPANY LIMITED 60
career henan chemical co 58
Chongqing Chemdad Co., Ltd 58

65576-45-6(Asenapine)Related 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
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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 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 ORG 5222;ORG-5222;ORG5222 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 Saphris Asenapine (Org 5222) 65576-45-6 C17H16CINOC4H4O4 Aromatics Heterocycles Intermediates & Fine Chemicals Pharmaceuticals