CAS 132810-10-7|Blonanserin

Introduction：Basic information about CAS 132810-10-7|Blonanserin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Blonanserin BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles25
6. Synonyms

Common Name	Blonanserin
CAS Number	132810-10-7	Molecular Weight	367.503
Density	1.1±0.1 g/cm3	Boiling Point	540.8±50.0 °C at 760 mmHg
Molecular Formula	C₂₃H₃₀FN₃	Melting Point	117-119°C
MSDS	ChineseUSA	Flash Point	280.9±30.1 °C
Symbol	GHS07	Signal Word	Warning

Names

Name	Blonanserin
Synonym	More Synonyms

Blonanserin BiologicalActivity

Description	Blonanserin(AD-5423) is a D2/5-HT2 receptor antagonist, atypical antipsychotic. Target: D2 receptor; 5-HT2 receptorBlonanserin(AD-5423) is a relatively new atypical antipsychotic for the treatment of schizophrenia. Blonanserin belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors. Blonanserin has low affinity for 5-HT2C, adrenergic α1, histamine H1, and muscarinic M1 receptors, but displays relatively high affinity for 5-HT6 receptors [1]. AD-5423 bound preferentially to dopamine (DA)-D2 (Ki, 14.8 nM; cf. haloperidol, 8.79 nM; and clozapine, 149 nM) and serotonin (5-HT)-S2 (Ki, 3.98 nM; cf. haloperidol, 26.8 nM; and clozapine, 8.66 nM) receptors. It displayed low affinity for adrenaline (Ad)-alpha-1 (Ki, 56.3 nM) receptors and was virtually devoid of binding to DA-D1 (Ki, 2870 nM), 5-HT-S3, Ad-alpha-2, Ad-beta, muscarine, tau-aminobutyric acid and benzodiazepine receptors. In addition, AD-5423 was only a weak inhibitor of DA, 5-HT and noradrenaline uptake systems. AD-5423 (0.2-2 mg/kg p.o.) decreased exploratory activity in mice. AD-5423 (10 mg/kg p.o.), unlike haloperidol, did not antagonize SKF38393-induced vacuous oral movements in rats. Head twitches induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane in mice and by para-chloroamphetamine in rats were antagonized by AD-5423 at much lower doses (0.5-2 mg/kg p.o.) than those of haloperidol and clozapine [2].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorSignaling Pathways >>GPCR/G Protein >>Dopamine ReceptorSignaling Pathways >>Neuronal Signaling >>Dopamine ReceptorResearch Areas >>Neurological Disease
References	[1]. Tenjin, T., et al., Profile of blonanserin for the treatment of schizophrenia. Neuropsychiatr Dis Treat, 2013. 9: p. 587-94. [2]. Oka, M., et al., Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. J Pharmacol Exp Ther, 1993. 264(1): p. 158-65.

Description

Blonanserin(AD-5423) is a D2/5-HT2 receptor antagonist, atypical antipsychotic. Target: D2 receptor; 5-HT2 receptorBlonanserin(AD-5423) is a relatively new atypical antipsychotic for the treatment of schizophrenia. Blonanserin belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors. Blonanserin has low affinity for 5-HT2C, adrenergic α1, histamine H1, and muscarinic M1 receptors, but displays relatively high affinity for 5-HT6 receptors [1]. AD-5423 bound preferentially to dopamine (DA)-D2 (Ki, 14.8 nM; cf. haloperidol, 8.79 nM; and clozapine, 149 nM) and serotonin (5-HT)-S2 (Ki, 3.98 nM; cf. haloperidol, 26.8 nM; and clozapine, 8.66 nM) receptors. It displayed low affinity for adrenaline (Ad)-alpha-1 (Ki, 56.3 nM) receptors and was virtually devoid of binding to DA-D1 (Ki, 2870 nM), 5-HT-S3, Ad-alpha-2, Ad-beta, muscarine, tau-aminobutyric acid and benzodiazepine receptors. In addition, AD-5423 was only a weak inhibitor of DA, 5-HT and noradrenaline uptake systems. AD-5423 (0.2-2 mg/kg p.o.) decreased exploratory activity in mice. AD-5423 (10 mg/kg p.o.), unlike haloperidol, did not antagonize SKF38393-induced vacuous oral movements in rats. Head twitches induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane in mice and by para-chloroamphetamine in rats were antagonized by AD-5423 at much lower doses (0.5-2 mg/kg p.o.) than those of haloperidol and clozapine [2].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorSignaling Pathways >>GPCR/G Protein >>Dopamine ReceptorSignaling Pathways >>Neuronal Signaling >>Dopamine ReceptorResearch Areas >>Neurological Disease

References

[1]. Tenjin, T., et al., Profile of blonanserin for the treatment of schizophrenia. Neuropsychiatr Dis Treat, 2013. 9: p. 587-94.

[2]. Oka, M., et al., Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. J Pharmacol Exp Ther, 1993. 264(1): p. 158-65.

Chemical & Physical Properties

Density	1.1±0.1 g/cm3
Boiling Point	540.8±50.0 °C at 760 mmHg
Melting Point	117-119°C
Molecular Formula	C₂₃H₃₀FN₃
Molecular Weight	367.503
Flash Point	280.9±30.1 °C
Exact Mass	367.242371
PSA	19.37000
LogP	6.03
Appearance of Characters	white to off-white
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.557
InChIKey	XVGOZDAJGBALKS-UHFFFAOYSA-N
SMILES	CCN1CCN(c2cc(-c3ccc(F)cc3)c3c(n2)CCCCCC3)CC1
Storage condition	Refrigerator
Water Solubility	DMSO: ≥10mg/mL

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H413
Hazard Codes	Xn
Risk Phrases	22
RIDADR	NONH for all modes of transport
RTECS	GY0175140

Articles25

Asenapine, blonanserin, iloperidone, lurasidone, and sertindole: distinctive clinical characteristics of 5 novel atypical antipsychotics.

Clin. Neuropharmacol. 36(6) , 223-38, (2013)

Schizophrenia is a serious, chronic, and devastating mental illness with a substantial impact on psychological, physical, social, and economical areas of an individual and society. To treat such criti...

Blonanserin in the treatment of delirium.

Psychiatry Clin. Neurosci. 65(4) , 389-91, (2011)

The purpose of the present study was to provide preliminary data on the usefulness and safety of blonanserin for patients with delirium in the intensive care unit (ICU). The charts of 32 consecutive p...

Five Alzheimer's disease cases with refractory behavioural psychological symptoms of dementia treated with blonanserin.

Psychogeriatrics 10(4) , 198-200, (2010)

The aim of the present study was to determine the efficacy, side-effects and tolerability of blonanserin for treating refractory behavioural psychological symptoms of dementia (BPSD). The present stud...

Synonyms

2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine

2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine

Lonasen

Blonanserin

Cycloocta[b]pyridine, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-

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