BLONANSERIN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H30FN3
Molecular Weight	367.5028
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(F)C=C4

InChI

InChIKey=XVGOZDAJGBALKS-UHFFFAOYSA-N

InChI=1S/C23H30FN3/c1-2-26-13-15-27(16-14-26)23-17-21(18-9-11-19(24)12-10-18)20-7-5-3-4-6-8-22(20)25-23/h9-12,17H,2-8,13-16H2,1H3

HIDE SMILES / InChI

Molecular Formula	C23H30FN3
Molecular Weight	367.5028
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647

Blonanserin is an antagonist of dopamine and serotonin receptors developed for the treatment of schizophrenia. Blonanserin was approved in Japan and Korea, but was never marketed in the USA.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647	Antagonist 2778	0.142 nM [Ki]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647	Antagonist 2778	0.494 nM [Ki]
Serotonin 2a (5-HT2a) receptor 231 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647	Antagonist 2778	0.812 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 298 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647	Primary		Approved 8429	LONASEN Approved Use Schizophrenia. Launch Date 1.25971202E12

PubMed

Title	Date	PubMed
		252160945
Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties.	1993 Jan	8093723
Blonanserin. AD 5423.	2002	12516946
The effects of neuroleptics on the GABA-induced Cl- current in rat dorsal root ganglion neurons: differences between some neuroleptics.	2002 Mar	11906969
Gateways to clinical trials.	2002 Nov	12616707
Crystal structure of an antipsychotic agent, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (blonanserin).	2002 Nov	12458724
Effect of AD-5423 on animal models of schizophrenia: phencyclidine-induced behavioral changes in mice.	2003 Feb 10	12598744
Atypical properties of several classes of antipsychotic drugs on the basis of differential induction of Fos-like immunoreactivity in the rat brain.	2004 Nov 26	15519367
Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.	2005 Feb 15	15686911
[Pharmacological profiles and clinical effects of blonanserin (Lonasen) on schizophrenia].	2008 Dec	19075531
The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study.	2009	19552488
Efficacy of blonanserin in combination therapy for treatment-resistant depression.	2009 Aug	19659567
Sensitive analysis of blonanserin, a novel antipsychotic agent, in human plasma by ultra-performance liquid chromatography-tandem mass spectrometry.	2010	20953055
Beneficial effects of loxapine on agitation and breathing patterns during weaning from mechanical ventilation.	2010	20459867
Fluvoxamine for blonanserin-associated akathisia in patients with schizophrenia: report of five cases.	2010 Apr 24	20416096
Atypical antipsychotic properties of blonanserin, a novel dopamine D2 and 5-HT2A antagonist.	2010 Aug	20460137
Five Alzheimer's disease cases with refractory behavioural psychological symptoms of dementia treated with blonanserin.	2010 Dec	21159055
Blonanserin: a review of its use in the management of schizophrenia.	2010 Jan	20030420
Efficacy and tolerability of Blonanserin in the patients with schizophrenia: a randomized, double-blind, risperidone-compared trial.	2010 Jul	20661022
The relationship between the daily dose, the plasma concentration of blonanserin, and its plasma anti-dopamine D2 and anti-serotonin 5-HT2A activity.	2010 Jun-Jul	20521325
Case of delirium complicated with pneumonia that improved with blonanserin administration.	2010 Oct	20923437
Adjunctive treatment with low-dosage aripiprazole for blonanserin-induced hyperprolactinemia in a female patient with schizophrenia.	2010 Oct 1	20647025
Effect of dose timing in relation to food intake on systemic exposure to blonanserin.	2010 Sep	20490472
Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake.	2013 Mar	23417765

Patents

Sample Use Guides

In Vivo Use Guide

Initial dose is 8 mg/day divided in 2 doses; maintenance dose is 8–16 mg/day divided in 2 doses; maximum dose is 24 mg/day.

Route of Administration: Oral

In Vitro Use Guide

Rat dorsal root ganglion neurons were treated with increasing concentrations of blonanserin (0.01-100 uM). Blonanserin at 30 and 50 uM potentiated the GABA (3 uM)-current to 170.1 and 192.0 % of the control current, respectively.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 17:35:25 UTC 2023` Edited by `admin` on `Sat Dec 16 17:35:25 UTC 2023`
Record UNII	AQ316B4F8C
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BLONANSERIN

Official Name

English

BLONANSERIN [JAN]

Common Name

English

Blonanserin [WHO-DD]

Common Name

English

blonanserin [INN]

Common Name

English

DSP-5423

Code

English

BLONANSERIN [MI]

Common Name

English

2-(4-ETHYL-1-PIPERAZINYL)-4-(P-FLUOROPHENYL)-5,6,7,8,9,10-HEXAHYDROCYCLOOCTA(B)PYRIDINE

Common Name

English

BLONANSERIN [MART.]

Common Name

English

2-(4-ETHYLPIPERAZIN-1-YL)-4-(4-FLUOROPHENYL)-5,6,7,8,9,10-HEXAHYDROCYCLOOCTA(B)PYRIDINE

Systematic Name

English

AD-5423

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C66885