Asenapine

Modify Date: 2024-01-03 20:06:09

Asenapine structure	Common Name	Asenapine
	CAS Number	65576-45-6	Molecular Weight	285.768
	Density	1.2±0.1 g/cm3	Boiling Point	357.9±42.0 °C at 760 mmHg
	Molecular Formula	C₁₇H₁₆ClNO	Melting Point	N/A
	MSDS	N/A	Flash Point	170.2±27.9 °C

Use of Asenapine

Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. IC50 Value: 0.25-1.2 nM(Ki for adrenergic receptor); 0.03-4.0 nM(Ki for 5-HT receptor)Target: 5-HT Receptor; Adrenergic ReceptorAsenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic. Asenapine has a broad receptor affinity profile for most serotonergic, dopaminergic, and adrenergic receptors, with no appreciable affinity for muscarinic receptors. Asenapine may be a helpful treatment option for patients with schizophrenia when weight gain, dyslipidemia, and endocrine abnormalities are a concern.

Name	Asenapine
Synonym	More Synonyms

Description	Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. IC50 Value: 0.25-1.2 nM(Ki for adrenergic receptor); 0.03-4.0 nM(Ki for 5-HT receptor)Target: 5-HT Receptor; Adrenergic ReceptorAsenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic. Asenapine has a broad receptor affinity profile for most serotonergic, dopaminergic, and adrenergic receptors, with no appreciable affinity for muscarinic receptors. Asenapine may be a helpful treatment option for patients with schizophrenia when weight gain, dyslipidemia, and endocrine abnormalities are a concern.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Neurological Disease
References	[1]. Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40. [2]. Tarazi FI, Shahid M. Asenapine maleate: a new drug for the treatment of schizophrenia and bipolar mania. Drugs Today (Barc). 2009 Dec;45(12):865-76. [3]. Elsworth JD, Groman SM, Jentsch JD et al. Asenapine effects on cognitive and monoamine dysfunction elicited by subchronic phencyclidine administration. Neuropharmacology. 2012 Mar;62(3):1442-52. [4]. Potkin SG. Asenapine: a clinical overview. J Clin Psychiatry. 2011;72 Suppl 1:14-8. [5]. Shahid M, Walker GB, Zorn SH, Wong EH. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. [6]. Asenapine

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

References

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

[2]. Tarazi FI, Shahid M. Asenapine maleate: a new drug for the treatment of schizophrenia and bipolar mania. Drugs Today (Barc). 2009 Dec;45(12):865-76.

[3]. Elsworth JD, Groman SM, Jentsch JD et al. Asenapine effects on cognitive and monoamine dysfunction elicited by subchronic phencyclidine administration. Neuropharmacology. 2012 Mar;62(3):1442-52.

[4]. Potkin SG. Asenapine: a clinical overview. J Clin Psychiatry. 2011;72 Suppl 1:14-8.

[5]. Shahid M, Walker GB, Zorn SH, Wong EH. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.

[6]. Asenapine

Density	1.2±0.1 g/cm3
Boiling Point	357.9±42.0 °C at 760 mmHg
Molecular Formula	C₁₇H₁₆ClNO
Molecular Weight	285.768
Flash Point	170.2±27.9 °C
Exact Mass	285.092041
PSA	12.47000
LogP	4.31
Vapour Pressure	0.0±0.8 mmHg at 25°C
Index of Refraction	1.610
Storage condition	Store at +4°C

HS Code	2934999090

Precursor 10
CAS#:129385-59-7 trans-(+/-)-11-... CAS#:85650-56-2 Asenapine Maleate CAS#:2444-36-2 2-Chlorophenyla... CAS#:57486-68-7 Methyl (2-chlor...
CAS#:934996-79-9 2,3-Dihydro-1-o... CAS#:106-48-9 4-Chlorophenol CAS#:25563-04-6 2-(4-Chlorophen... CAS#:1035404-17-1 Ethyl 2-(2-(2-(...
CAS#:611-17-6 1-(Bromomethyl)... CAS#:29074-98-4 Diethyl (2-Chlo...
DownStream 2
CAS#:85650-56-2 Asenapine Maleate CAS#:128915-56-0 N-desmethylasenapine