Asenapine hydrochloride

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

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.

Name	Asenapine hydrochloride
Synonym	More Synonyms

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	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
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.

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

cs-1053

Asenapine (hydrochloride)

Asenapine hydrochloride

Use of Asenapine hydrochloride

Names

Asenapine hydrochloride Biological Activity

Chemical & Physical Properties

Synonyms