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
| 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 |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23766647
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 | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647 |
0.142 nM [Ki] | ||
Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647 |
0.494 nM [Ki] | ||
Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23766647 |
0.812 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | LONASEN Approved UseSchizophrenia. Launch Date2009 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.1 ng/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.26 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.33 ng/mL |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.131 ng/mL |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.3 ng/mL |
6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.417 ng/mL |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.946 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.679 ng/mL |
12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.538 ng/mL |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
0.317 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
0.88 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.195 ng/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.51 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.38 ng/mL |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.46 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.21 ng/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.1457 ng/mL |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.4399 ng/mL |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.4153 ng/mL |
25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.1293 ng/mL |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.338 ng/mL |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
62.9 pg/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
136.9 pg/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.39 ng × h/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.23 ng × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.52 ng × h/mL |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.84 ng × h/mL |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.91 ng × h/mL |
6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.6 ng × h/mL |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.13 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.71 ng × h/mL |
12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.06 ng × h/mL |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2.14 ng × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.6 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
15.5 ng × h/mL |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.3 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
52.2 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.8984 ng × h/mL |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.6219 ng × h/mL |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
13.6851 ng × h/mL |
25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.4432 ng × h/mL |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.766 ng × h/mL |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
355.9 pg × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
833.9 pg × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
13 h |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
8.26 h |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
12.4 h |
6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.1 h |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
19 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
15.5 h |
12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
63.3 h |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
12.5 h |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.5 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
7.7 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.7 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
14.1 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.6 h |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4.8 h |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
7 h |
25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
12.6 h |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8 h |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BLONANSERIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.12% |
BLONANSERIN serum | Homo sapiens |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 1 times / day multiple, transdermal Highest studied dose Dose: 80 mg, 1 times / day Route: transdermal Route: multiple Dose: 80 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
8 mg 1 times / day multiple, oral Studied dose Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake. | 2013-03 |
|
| Five Alzheimer's disease cases with refractory behavioural psychological symptoms of dementia treated with blonanserin. | 2010-12 |
|
| Adjunctive treatment with low-dosage aripiprazole for blonanserin-induced hyperprolactinemia in a female patient with schizophrenia. | 2010-10-01 |
|
| Case of delirium complicated with pneumonia that improved with blonanserin administration. | 2010-10 |
|
| Effect of dose timing in relation to food intake on systemic exposure to blonanserin. | 2010-09 |
|
| Atypical antipsychotic properties of blonanserin, a novel dopamine D2 and 5-HT2A antagonist. | 2010-08 |
|
| Efficacy and tolerability of Blonanserin in the patients with schizophrenia: a randomized, double-blind, risperidone-compared trial. | 2010-07 |
|
| The relationship between the daily dose, the plasma concentration of blonanserin, and its plasma anti-dopamine D2 and anti-serotonin 5-HT2A activity. | 2010-06-04 |
|
| Fluvoxamine for blonanserin-associated akathisia in patients with schizophrenia: report of five cases. | 2010-04-24 |
|
| Blonanserin: a review of its use in the management of schizophrenia. | 2010-01 |
|
| Sensitive analysis of blonanserin, a novel antipsychotic agent, in human plasma by ultra-performance liquid chromatography-tandem mass spectrometry. | 2010 |
|
| Beneficial effects of loxapine on agitation and breathing patterns during weaning from mechanical ventilation. | 2010 |
|
| Efficacy of blonanserin in combination therapy for treatment-resistant depression. | 2009-08 |
|
| The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study. | 2009 |
|
| [Pharmacological profiles and clinical effects of blonanserin (Lonasen) on schizophrenia]. | 2008-12 |
|
| Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent. | 2005-02-15 |
|
| Atypical properties of several classes of antipsychotic drugs on the basis of differential induction of Fos-like immunoreactivity in the rat brain. | 2004-11-26 |
|
| Effect of AD-5423 on animal models of schizophrenia: phencyclidine-induced behavioral changes in mice. | 2003-02-10 |
|
| Gateways to clinical trials. | 2002-11 |
|
| Crystal structure of an antipsychotic agent, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (blonanserin). | 2002-11 |
|
| The effects of neuroleptics on the GABA-induced Cl- current in rat dorsal root ganglion neurons: differences between some neuroleptics. | 2002-03 |
|
| Blonanserin. AD 5423. | 2002 |
|
| Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. | 1993-01 |
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11906969
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
Edited
Wed Apr 02 09:19:40 GMT 2025
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Wed Apr 02 09:19:40 GMT 2025
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| Record UNII |
AQ316B4F8C
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| Record Status |
Validated (UNII)
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NCI_THESAURUS |
C66885
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m2590
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125564
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Blonanserin
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AQ316B4F8C
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7563
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