Identification

Name
Blonanserin
Accession Number
DB09223
Type
Small Molecule
Groups
Approved, Investigational
Description

Blonanserin is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As with many second-generation (atypical) antipsychotics it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics such as haloperidol.

Structure
Thumb
Synonyms
Not Available
External IDs
AD 5423 / AD-5423
Categories
UNII
AQ316B4F8C
CAS number
132810-10-7
Weight
Average: 367.512
Monoisotopic: 367.242376141
Chemical Formula
C23H30FN3
InChI Key
XVGOZDAJGBALKS-UHFFFAOYSA-N
InChI
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
IUPAC Name
1-ethyl-4-[4-(4-fluorophenyl)-5H,6H,7H,8H,9H,10H-cycloocta[b]pyridin-2-yl]piperazine
SMILES
CCN1CCN(CC1)C1=NC2=C(CCCCCC2)C(=C1)C1=CC=C(F)C=C1

Pharmacology

Indication

Used for the treatment of schizophrenia [4].

Pharmacodynamics

Blonanserin antagonizes dopamine and serotonin receptors to reduce symptoms of schizophrenia [2].

Mechanism of action

Blonanserin binds to and inhibits dopamine receptors D2 and D3 as well as the serotonin receptor 5-HT2A with high affinity [2]. Blonanserin has low affinity for other dopamine and serotonin receptors as well as muscarinic, adrenergic, and histamine receptors. This reduces dopaminergic and serotonergic neurotransmission which is thought to produce a reduction in positive and negative symptoms of schizophrenia respectively.

TargetActionsOrganism
AD(2) dopamine receptor
antagonist
Human
AD(3) dopamine receptor
antagonist
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
Absorption

Blonanserin has a Tmax of 1.5 h and a bioavailablity of 55% [1, 2]. Tmax has been observed to be prolonged and relative bioavailability increased when administered with food [1].

Volume of distribution

Blonanserin has a Vc of 9500 L and a Vt of 8560 L for a total Vd of 18060 L [1].

Protein binding

Blonanserin is over 99.7% bound to plasma proteins [2] . Serum albumin is the primary binder.

Metabolism

Blonanserin is mainly metabolized by CYP3A4 [2]. It undergoes hydoxylation of the cyclooctane ring as well as N-oxidation and N-deethylation of the piperazine ring. The N-deethylated and hydroxylated metabolites are active but to a lesser degree than the parent drug.

Route of elimination

57% of blonanserin is excreted in the urine and 30% in the feces [2]. Only 5% of the drug in the feces is the parent drug with no parent drug excreted through the urine.

Half life

Blonanserin has a half life of elimination of 10.7-16.2 h [2].

Clearance

Blonanserin has a clearance of 1230 L/h [1].

Toxicity

Oral LD50 of >500 mg/kg in mice [5].

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
Acetyl sulfisoxazoleThe metabolism of Blonanserin can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AmantadineThe therapeutic efficacy of Amantadine can be decreased when used in combination with Blonanserin.Approved
AmikacinThe risk or severity of adverse effects can be increased when Blonanserin is combined with Amikacin.Approved, Investigational, Vet Approved
AmiodaroneThe metabolism of Blonanserin can be decreased when combined with Amiodarone.Approved, Investigational
ApalutamideThe serum concentration of Blonanserin can be decreased when it is combined with Apalutamide.Approved, Investigational
ApomorphineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Blonanserin.Approved, Investigational
AprepitantThe serum concentration of Blonanserin can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe metabolism of Blonanserin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Blonanserin can be decreased when combined with Atomoxetine.Approved
BenzphetamineThe risk or severity of serotonin syndrome can be increased when Blonanserin is combined with Benzphetamine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Blonanserin.Approved
BoceprevirThe metabolism of Blonanserin can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Blonanserin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Blonanserin can be decreased when it is combined with Bosentan.Approved, Investigational
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Blonanserin.Approved, Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Blonanserin.Approved
BupropionThe risk or severity of adverse effects can be increased when Bupropion is combined with Blonanserin.Approved
CarbamazepineThe metabolism of Blonanserin can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Blonanserin can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Blonanserin.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Blonanserin.Approved
ClarithromycinThe metabolism of Blonanserin can be decreased when combined with Clarithromycin.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Blonanserin.Approved, Investigational
ClindamycinThe risk or severity of adverse effects can be increased when Clindamycin is combined with Blonanserin.Approved, Vet Approved
ClotrimazoleThe metabolism of Blonanserin can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Blonanserin can be decreased when combined with Cobicistat.Approved
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Blonanserin.Approved, Illicit
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Blonanserin.Approved, Investigational
CrizotinibThe metabolism of Blonanserin can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Blonanserin can be decreased when combined with Curcumin.Approved, Investigational
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Blonanserin.Approved
CyclosporineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Blonanserin can be decreased when it is combined with Dabrafenib.Approved, Investigational
DarunavirThe metabolism of Blonanserin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Blonanserin can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Blonanserin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Blonanserin can be decreased when combined with Delavirdine.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Desvenlafaxine.Approved, Investigational
DeutetrabenazineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Deutetrabenazine.Approved, Investigational
DexamethasoneThe serum concentration of Blonanserin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Blonanserin.Approved
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Blonanserin.Approved
DiethylpropionBlonanserin may decrease the stimulatory activities of Diethylpropion.Approved, Illicit
DihydroergotamineThe metabolism of Blonanserin can be decreased when combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe metabolism of Blonanserin can be decreased when combined with Diltiazem.Approved, Investigational
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Blonanserin.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Blonanserin.Approved, Investigational
DotarizineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Dotarizine.Investigational
DoxycyclineThe metabolism of Blonanserin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Blonanserin.Approved, Vet Approved
DronedaroneThe metabolism of Blonanserin can be decreased when combined with Dronedarone.Approved
EnzalutamideThe serum concentration of Blonanserin can be decreased when it is combined with Enzalutamide.Approved
EperisoneThe risk or severity of adverse effects can be increased when Eperisone is combined with Blonanserin.Approved, Investigational
ErythromycinThe metabolism of Blonanserin can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EthanolBlonanserin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Blonanserin.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Blonanserin.Approved
FentanylThe risk or severity of serotonin syndrome can be increased when Fentanyl is combined with Blonanserin.Approved, Illicit, Investigational, Vet Approved
FluconazoleThe metabolism of Blonanserin can be decreased when combined with Fluconazole.Approved, Investigational
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Blonanserin.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Fluoxetine.Approved, Vet Approved
FluspirileneThe risk or severity of adverse effects can be increased when Blonanserin is combined with Fluspirilene.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Blonanserin.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Blonanserin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Blonanserin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Blonanserin can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Blonanserin can be increased when it is combined with Fusidic Acid.Approved, Investigational
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Blonanserin.Approved, Investigational
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Blonanserin.Approved, Investigational
HydrocodoneBlonanserin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Blonanserin.Approved
IdelalisibThe metabolism of Blonanserin can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Blonanserin can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Blonanserin can be decreased when combined with Indinavir.Approved
IsavuconazoleThe serum concentration of Blonanserin can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Blonanserin can be decreased when combined with Isavuconazonium.Approved, Investigational
ItraconazoleThe metabolism of Blonanserin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Blonanserin can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Blonanserin can be decreased when combined with Ketoconazole.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Blonanserin.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Blonanserin.Approved, Investigational
LevodopaThe therapeutic efficacy of Levodopa can be decreased when used in combination with Blonanserin.Approved
LopinavirThe metabolism of Blonanserin can be decreased when combined with Lopinavir.Approved
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Blonanserin.Approved, Investigational
LorpiprazoleThe serum concentration of Blonanserin can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe metabolism of Blonanserin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Blonanserin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Blonanserin can be increased when combined with Lumacaftor.Approved
Magnesium carbonateThe risk or severity of adverse effects can be increased when Blonanserin is combined with Magnesium carbonate.Approved, Investigational
Magnesium citrateThe risk or severity of adverse effects can be increased when Blonanserin is combined with Magnesium citrate.Approved
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Blonanserin is combined with Magnesium hydroxide.Approved, Investigational
Magnesium sulfateThe therapeutic efficacy of Blonanserin can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
Magnesium TrisilicateThe risk or severity of adverse effects can be increased when Blonanserin is combined with Magnesium Trisilicate.Approved
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Blonanserin.Approved
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with Blonanserin.Approved
MethylphenidateThe risk or severity of adverse effects can be increased when Blonanserin is combined with Methylphenidate.Approved, Investigational
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Blonanserin.Approved, Investigational
MetoclopramideThe risk or severity of serotonin syndrome can be increased when Metoclopramide is combined with Blonanserin.Approved, Investigational
MibefradilThe metabolism of Blonanserin can be decreased when combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe metabolism of Blonanserin can be decreased when combined with Miconazole.Approved, Investigational, Vet Approved
MifepristoneThe serum concentration of Blonanserin can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Blonanserin can be decreased when it is combined with Mitotane.Approved
NefazodoneThe metabolism of Blonanserin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Blonanserin can be decreased when combined with Nelfinavir.Approved
NeomycinThe risk or severity of adverse effects can be increased when Blonanserin is combined with Neomycin.Approved, Vet Approved
NetupitantThe serum concentration of Blonanserin can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Blonanserin can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Blonanserin can be decreased when combined with Nicardipine.Approved, Investigational
NilotinibThe metabolism of Blonanserin can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Blonanserin can be decreased when combined with Olaparib.Approved
OndansetronThe risk or severity of serotonin syndrome can be increased when Ondansetron is combined with Blonanserin.Approved
OsimertinibThe serum concentration of Blonanserin can be increased when it is combined with Osimertinib.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Blonanserin.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Blonanserin.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Blonanserin can be increased when it is combined with Palbociclib.Approved, Investigational
ParomomycinThe risk or severity of adverse effects can be increased when Blonanserin is combined with Paromomycin.Approved, Investigational
ParoxetineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Paroxetine.Approved, Investigational
PenfluridolThe risk or severity of adverse effects can be increased when Penfluridol is combined with Blonanserin.Experimental
PentobarbitalThe metabolism of Blonanserin can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PhenobarbitalThe metabolism of Blonanserin can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe metabolism of Blonanserin can be increased when combined with Phenytoin.Approved, Vet Approved
PiribedilThe therapeutic efficacy of Piribedil can be decreased when used in combination with Blonanserin.Investigational
PitolisantThe serum concentration of Blonanserin can be decreased when it is combined with Pitolisant.Approved, Investigational
Polymyxin B SulfateThe risk or severity of adverse effects can be increased when Blonanserin is combined with Polymyxin B Sulfate.Approved, Vet Approved
PosaconazoleThe metabolism of Blonanserin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleBlonanserin may increase the sedative activities of Pramipexole.Approved, Investigational
PregabalinThe therapeutic efficacy of Blonanserin can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrimidoneThe metabolism of Blonanserin can be increased when combined with Primidone.Approved, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Blonanserin.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Blonanserin.Approved, Investigational
PseudoephedrineThe risk or severity of adverse effects can be increased when Pseudoephedrine is combined with Blonanserin.Approved
PyrantelThe risk or severity of adverse effects can be increased when Pyrantel is combined with Blonanserin.Approved, Vet Approved
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Blonanserin.Approved
RanolazineThe metabolism of Blonanserin can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Blonanserin can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Blonanserin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Blonanserin can be increased when combined with Rifapentine.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Blonanserin.Approved
RopiniroleBlonanserin may increase the sedative activities of Ropinirole.Approved, Investigational
RotigotineThe therapeutic efficacy of Rotigotine can be decreased when used in combination with Blonanserin.Approved
RucaparibThe metabolism of Blonanserin can be decreased when combined with Rucaparib.Approved, Investigational
SaquinavirThe metabolism of Blonanserin can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Blonanserin can be decreased when used in combination with Sarilumab.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Blonanserin.Approved, Investigational
SildenafilThe metabolism of Blonanserin can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Blonanserin can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Blonanserin can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Blonanserin can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Blonanserin can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Blonanserin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Blonanserin.Approved, Investigational
TelaprevirThe metabolism of Blonanserin can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Blonanserin can be decreased when combined with Telithromycin.Approved
TetracyclineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Tetracycline.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with Blonanserin.Investigational
TiclopidineThe metabolism of Blonanserin can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Blonanserin can be decreased when it is combined with Tocilizumab.Approved
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Blonanserin.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Blonanserin.Approved, Investigational
TrimethadioneThe risk or severity of adverse effects can be increased when Trimethadione is combined with Blonanserin.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Blonanserin.Approved, Investigational
VancomycinThe risk or severity of adverse effects can be increased when Blonanserin is combined with Vancomycin.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Blonanserin.Approved
VemurafenibThe serum concentration of Blonanserin can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Blonanserin is combined with Venlafaxine.Approved
VerapamilThe metabolism of Blonanserin can be decreased when combined with Verapamil.Approved
VinpocetineThe risk or severity of adverse effects can be increased when Vinpocetine is combined with Blonanserin.Investigational
VoriconazoleThe metabolism of Blonanserin can be decreased when combined with Voriconazole.Approved, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Blonanserin.Approved
ZiprasidoneThe metabolism of Blonanserin can be decreased when combined with Ziprasidone.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Blonanserin.Approved, Investigational
ZolpidemBlonanserin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Blonanserin.Approved, Investigational
Food Interactions
Not Available

References

General References
  1. Wen YG, Shang DW, Xie HZ, Wang XP, Ni XJ, Zhang M, Lu W, Qiu C, Liu X, Li FF, Li X, Luo FT: Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake. Hum Psychopharmacol. 2013 Mar;28(2):134-41. doi: 10.1002/hup.2290. Epub 2013 Feb 18. [PubMed:23417765]
  2. Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000. [PubMed:20030420]
  3. Zhou Y, Liu M, Jiang J, Wang H, Hu P: Simultaneous determination of blonanserin and its four metabolites in human plasma using ultra-performance liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Nov 15;939:59-66. doi: 10.1016/j.jchromb.2013.09.007. Epub 2013 Sep 18. [PubMed:24099858]
  4. Blonanserin Approval Announcement [Link]
  5. ChemIDPlus: Blonanserin [Link]
External Links
KEGG Drug
D01176
PubChem Compound
125564
PubChem Substance
310265129
ChemSpider
111697
BindingDB
50160807
ChEBI
31296
ChEMBL
CHEMBL178803
Wikipedia
Blonanserin
MSDS
Download (42.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentSchizophrenic Disorders1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP5.266MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.0359 mg/mLALOGPS
logP5.76ALOGPS
logP5.67ChemAxon
logS-4ALOGPS
pKa (Strongest Basic)7.97ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area19.37 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity111.05 m3·mol-1ChemAxon
Polarizability42.8 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001j-0961000000-b7df0ccb917e6467df2e
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014j-0089000000-88be7b13b01a432d7bda

Taxonomy

Description
This compound belongs to the class of organic compounds known as pyridinylpiperazines. These are compounds containing a pyridinylpiperazine skeleton, which consists of a pyridine linked (not fused) to a piperazine by a bond by a single bond that is not part of a ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Pyridinylpiperazines
Alternative Parents
Phenylpyridines / N-arylpiperazines / Dialkylarylamines / N-alkylpiperazines / Fluorobenzenes / Aminopyridines and derivatives / Imidolactams / Aryl fluorides / Heteroaromatic compounds / Trialkylamines
show 4 more
Substituents
4-phenylpyridine / Pyridinylpiperazine / N-arylpiperazine / Dialkylarylamine / Aminopyridine / Fluorobenzene / Halobenzene / N-alkylpiperazine / Aryl fluoride / Pyridine
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000. [PubMed:20030420]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000. [PubMed:20030420]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000. [PubMed:20030420]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Curator comments
Blonanserin appears to be a sensitive substrate with AUC increasing 13-16 fold with exposure to strong CYP3A4 inhibitors.
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000. [PubMed:20030420]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000. [PubMed:20030420]

Drug created on October 22, 2015 14:10 / Updated on August 02, 2018 06:15