Blonanserin

Names

[ Name ]:
Blonanserin

[Synonym ]:
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-

Biological Activity

[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 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

[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.

[Related Small Molecules]

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

[ Storage condition ]:
Refrigerator

[ Water Solubility ]:
DMSO: ≥10mg/mL

MSDS

Click to get detail MSDS

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

Articles

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...