BLONANSERIN

Possibly Marketed Outside US

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

SMILES

CCN1CCN(CC1)C2=CC(C3=CC=C(F)C=C3)=C4CCCCCCC4=N2

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	MOL RATIO 1 MOL RATIO (average)

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

Description

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 311	Antagonist 2,849	0.142 nM [Ki]
Dopamine D3 receptor 97	Antagonist 2,849	0.494 nM [Ki]
Serotonin 2a (5-HT2a) receptor 237	Antagonist 2,849	0.812 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 305	Primary		Approved 8,583	LONASEN

C_max

Value	Dose	Analyte	Population
0.1 ng/mL	1 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.26 ng/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.33 ng/mL	4 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.131 ng/mL	4 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.3 ng/mL	6 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.417 ng/mL	8 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.946 ng/mL	10 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.679 ng/mL	12 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.538 ng/mL	2 mg 2 times / day steady-state, oral	BLONANSERIN plasma	Homo sapiens
0.317 ng/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.88 ng/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.195 ng/mL	5 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.51 ng/mL	10 mg single, oral	BLONANSERIN plasma	Homo sapiens
3.38 ng/mL	25 mg single, oral	BLONANSERIN plasma	Homo sapiens
5.46 ng/mL	40 mg single, oral	BLONANSERIN plasma	Homo sapiens
8.21 ng/mL	50 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.1457 ng/mL	5 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
0.4399 ng/mL	10 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
2.4153 ng/mL	25 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
0.1293 ng/mL	5 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
0.338 ng/mL	10 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
62.9 pg/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
136.9 pg/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
0.39 ng × h/mL	1 mg single, oral	BLONANSERIN plasma	Homo sapiens
1.23 ng × h/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
2.52 ng × h/mL	4 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.84 ng × h/mL	4 mg single, oral	BLONANSERIN plasma	Homo sapiens
1.91 ng × h/mL	6 mg single, oral	BLONANSERIN plasma	Homo sapiens
2.6 ng × h/mL	8 mg single, oral	BLONANSERIN plasma	Homo sapiens
6.13 ng × h/mL	10 mg single, oral	BLONANSERIN plasma	Homo sapiens
4.71 ng × h/mL	12 mg single, oral	BLONANSERIN plasma	Homo sapiens
3.06 ng × h/mL	2 mg 2 times / day steady-state, oral	BLONANSERIN plasma	Homo sapiens
2.14 ng × h/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
4.6 ng × h/mL	10 mg single, oral	BLONANSERIN plasma	Homo sapiens
15.5 ng × h/mL	25 mg single, oral	BLONANSERIN plasma	Homo sapiens
22.3 ng × h/mL	40 mg single, oral	BLONANSERIN plasma	Homo sapiens
52.2 ng × h/mL	50 mg single, oral	BLONANSERIN plasma	Homo sapiens
0.8984 ng × h/mL	5 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
2.6219 ng × h/mL	10 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
13.6851 ng × h/mL	25 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
1.4432 ng × h/mL	5 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
2.766 ng × h/mL	10 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
355.9 pg × h/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
833.9 pg × h/mL	2 mg single, oral	BLONANSERIN plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
13 h	4 mg single, oral	BLONANSERIN plasma	Homo sapiens
8.26 h	4 mg single, oral	BLONANSERIN plasma	Homo sapiens
12.4 h	6 mg single, oral	BLONANSERIN plasma	Homo sapiens
11.1 h	8 mg single, oral	BLONANSERIN plasma	Homo sapiens
19 h	10 mg single, oral	BLONANSERIN plasma	Homo sapiens
15.5 h	12 mg single, oral	BLONANSERIN plasma	Homo sapiens
63.3 h	2 mg 2 times / day steady-state, oral	BLONANSERIN plasma	Homo sapiens
12.5 h	2 mg single, oral	BLONANSERIN plasma	Homo sapiens
4.5 h	10 mg single, oral	BLONANSERIN plasma	Homo sapiens
7.7 h	25 mg single, oral	BLONANSERIN plasma	Homo sapiens
8.7 h	40 mg single, oral	BLONANSERIN plasma	Homo sapiens
14.1 h	50 mg single, oral	BLONANSERIN plasma	Homo sapiens
5.6 h	5 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
4.8 h	10 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
7 h	25 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
12.6 h	5 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens
8 h	10 mg 1 times / day multiple, oral	BLONANSERIN plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.12%			BLONANSERIN serum	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
80 mg 1 times / day multiple, transdermal Highest studied dose	unhealthy, ADULT
8 mg 1 times / day multiple, oral Studied dose	healthy, ADULT

Showing 1 to 2 of 2 entries

Previous1Next

PubMed

Show entries

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
Fluvoxamine for blonanserin-associated akathisia in patients with schizophrenia: report of five cases.	2010 Apr 24	20416096
Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake.	2013 Mar	23417765

Showing 1 to 4 of 4 entries

Previous1Next

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
Record UNII	AQ316B4F8C
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

BLONANSERIN

Official Name

English

AD-5423

Preferred Name

English

BLONANSERIN [JAN]

Common Name

English

Blonanserin [WHO-DD]

Common Name

English

blonanserin [INN]

Common Name

English

Showing 1 to 5 of 10 entries

Previous1 2Next

Show entries

Classification Tree

Code System

Code

Agent Affecting Nervous System

NCI_THESAURUS

C66885

Showing 1 to 1 of 1 entries

Previous1Next

Show entries

Code System

Code

Type

Description

MERCK INDEX

m2590

PRIMARY

Merck Index

PUBCHEM

125564

PRIMARY

EVMPD

SUB05864MIG

PRIMARY

DRUG CENTRAL

388

PRIMARY

DRUG BANK

DB09223

PRIMARY

Showing 1 to 5 of 15 entries

Previous1 2 3Next

Show entries

Related Record

Type

Details


					19GBD6T9L7

D(2) DOPAMINE RECEPTOR

TARGET -> INHIBITOR

Amount:


					NQI5D806LC

5-HYDROXYTRYPTAMINE RECEPTOR 2A

TARGET -> INHIBITOR

Amount:


					G9XQ9S7T2F

D(3) DOPAMINE RECEPTOR

TARGET -> INHIBITOR

Amount:

Showing 1 to 3 of 3 entries

Previous1Next

Show entries

Related Record

Type

Details


					AQ316B4F8C

BLONANSERIN

ACTIVE MOIETY

Amount:

Showing 1 to 1 of 1 entries

Previous1Next

SMILES

InChI

Description<div class="info-popup-container"><div><span class="pop-sub-key ">Sources:&nbsp;</span><span class="pop-sub-val"><span class="ext-link"><a target="_self" href="https://www.ncbi.nlm.nih.gov/pubmed/23766647">https://www.ncbi.nlm.nih.gov/pubmed/23766647</a></span></span></div></div>

CNS Activity

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Funbound

Doses

PubMed

Patents

Sample Use Guides

Description

C_max

T_1/2

F_unbound