Asenapine Maleate

Modify Date: 2024-01-05 22:20:45

Asenapine Maleate Structure
Asenapine Maleate structure
 Common Name Asenapine Maleate
CAS Number 85650-56-2 Molecular Weight 401.84000
Density N/A Boiling Point 357.9ºC at 760 mmHg
Molecular Formula C21H20ClNO5 Melting Point 141-145°
MSDS Chinese USA Flash Point 170.2ºC
Symbol GHS02 GHS06 GHS08
GHS02, GHS06, GHS08		 Signal Word Danger

 Use of Asenapine Maleate


Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.

 Names

Name Asenapine maleate
Synonym More Synonyms

 Asenapine Maleate Biological Activity

Description Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
Related Catalog
Target

5-HT1A Receptor:2.5 nM (Ki)

5-HT2A Receptor:0.06 nM (Ki)

5-HT2C Receptor:0.03 nM (Ki)

5-HT7 Receptor:0.13 nM (Ki)

D2 Receptor:1.3 nM (Ki)

D3 Receptor:0.42 nM (Ki)

D4 Receptor:1.1 nM (Ki)

In Vitro Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors[2].
In Vivo Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats[3]. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice[4].
Animal Admin Rats: Asenapine maleate is suspended in 10% hydroxypropyl-β-cyclodextrin and administered in a volume of 1 mL/kg body weight . Rats are individually fear conditioned using electrical foot shock in a Skinner box. Animals are injected intraperitoneally (i.p.) with asenapine, clozapine, olanzapine, buspirone, or SB242084 at 30 min before freezing behaviour assessment[3]. Mice: Male ICR mice are repeatedly treated with 0.1 or 0.3mg/kg injections of asenapine and then tested in a battery of behavioural tests related to anxiety including the open-field test, elevated plus-maze (EPM), defensive marble burying and hyponeophagia tests[4].
References

[1]. Stoner SC, et al. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40.

[2]. Shahid M, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.

[3]. Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336.

[4]. Ene HM, et al. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91.

 Chemical & Physical Properties

Boiling Point 357.9ºC at 760 mmHg
Melting Point 141-145°
Molecular Formula C21H20ClNO5
Molecular Weight 401.84000
Flash Point 170.2ºC
Exact Mass 401.10300
PSA 87.07000
LogP 3.90820
Storage condition 2-8°C
Water Solubility H2O: ≥10mg/mL

 Safety Information

Symbol GHS02 GHS06 GHS08
GHS02, GHS06, GHS08
Signal Word Danger
Hazard Statements H225-H301 + H311 + H331-H370
Precautionary Statements P210-P260-P280-P301 + P310-P311
Hazard Codes Xn;N
Risk Phrases R22;R36/37/38;R50/53
Safety Phrases S26-S60-S61
RIDADR UN1230 - class 3 - PG 2 - Methanol, solution
HS Code 29339900

 Synthetic Route

 Articles4

More Articles
Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude.

J. Neurosci. 35 , 9580-94, (2015)

Due to its distinct pharmacological profile and lower incidence of adverse events compared with other opioids, buprenorphine is considered a safe option for pain and substitution therapy. However, des...

Asenapine maleate in situ forming biodegradable implant: an approach to enhance bioavailability.

Int. J. Pharm. 477(1-2) , 64-72, (2014)

Biodegradable injectable in-situ forming implants (ISFI) correspond to an alternative parenteral depot system to microspheres and surgical implants. Objective of present work was to formulate and eval...

Asenapine maleate: a new drug for the treatment of schizophrenia and bipolar mania.

Drugs Today (Barc) 45 , 865-76, (2009)

Schizophrenia and bipolar disorder are serious neuropsychiatric disorders with substantial health risks for patients that result in major socioeconomic burdens on society. Current therapeutic agents f...

 Synonyms

1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, (3aS,12bS)-, (2Z)-2-butenedioate (1:1)
trans-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole maleate
Asenapine maleate
Asenapine
(3aS,12bS)-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole (2Z)-2-butenedioate (1:1)
Saphris
Asenapine (maleate)
trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz-[2,3:6,7]oxepino[4,5-C]pyrrolidino maleate
Sycrest
trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz<2,3:6,7>oxepino<4,5-c>pyrrolidine maleate
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole maleate
(3aRS,12bRS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole (2Z)-2-butenedioate
1H-Dibenz(2,3:6,7)oxepino(4,5-c)pyrrole,5-chloro-2,3,3a,12b-tetrahydro-2-methyl-,(3aR,12bR)-rel-,(2Z)-2-butenedioate (1:1)
Top Suppliers:I want be here

Get all suppliers and price by the below link:

Asenapine Maleate suppliers

Price: $66/10mM*1mLinDMSO

Reference only. check more Asenapine Maleate price

Related Compounds: More...
(S,S)-Asenapine Maleate
135883-08-8
Saphris,Asenapine maleate
122872-03-1
Asenapine citrate
1411867-74-7
Asenapine 11-Hydroxysulfate
1399103-21-9
Asenapine PI-4
165890-07-3
Asenapine hydrochloride
1412458-61-7
Asenapine
65576-45-6
Asenapine-d3
1180843-72-4
Asenapine N-Oxide
128949-51-9
4-((Cyclohexylamino)methyl)benzoic acid hydrochloride
1158522-08-7
1-[(2,4-Dichlorophenyl)methyl]-N-(1,1-dimethylethyl)-2-methyl-1H-indole-3-methanamine
940364-43-2
2-Methoxy-6-(pyrazol-1-yl)-benzonitrile
134104-43-1
1H-3-Benzazepin-7-ol, 8-chloro-2,3,4,5-tetrahydro-5-(3-iodophenyl)-3-methyl-, (S)-
131615-57-1
(4-Methyl-tetrahydro-furan-2-yl)-methanol
6906-52-1
N-(1-cyanocyclopentyl)-2-[4-(4-fluorobenzenesulfonyl)-1,4-diazepan-1-yl]acetamide
930439-75-1
4,5,6,7-Tetrahydrobenzo[d]isoxazole-3-carbaldehyde
1018584-77-4
tert-Butyl-DL-alanine
1375289-11-4
4-amino-N-[2-tert-butyl-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-benzimidazol-5-yl]-N-ethylbenzenesulfonamide
849349-65-1
N-[3-(Aminooxy)propyl]-N-butyl-1-butanamine
127437-46-1
Chemsrc provides Asenapine Maleate(CAS#:85650-56-2) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Asenapine Maleate are included as well.>> amp version: Asenapine Maleate

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved