Asenapine hydrochloride

Modify Date: 2024-01-09 11:16:06

Asenapine hydrochloride Structure
Asenapine hydrochloride structure
Common Name Asenapine hydrochloride
CAS Number 1412458-61-7 Molecular Weight 322.22900
Density N/A Boiling Point N/A
Molecular Formula C17H17Cl2NO Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Asenapine hydrochloride


Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.

 Names

Name Asenapine hydrochloride
Synonym More Synonyms

 Asenapine hydrochloride Biological Activity

Description Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
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].
References

[1]. Stoner SC, Pace HA. 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

Molecular Formula C17H17Cl2NO
Molecular Weight 322.22900
Exact Mass 321.06900
PSA 12.47000
LogP 4.99840
Storage condition 2-8℃

 Synonyms

cs-1053
Asenapine (hydrochloride)
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