Blonanserin
Identification
- Generic Name
- Blonanserin
- DrugBank Accession Number
- DB09223
- Background
Blonanserin is an atypical antipsychotic approved in Japan in January, 2008. It offers improved tolerability as it lacks side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As a second-generation (atypical) antipsychotic, it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
- Weight
- Average: 367.512
Monoisotopic: 367.242376141 - Chemical Formula
- C23H30FN3
- Synonyms
- Blonanserin
- External IDs
- AD 5423
- AD-5423
Pharmacology
- Indication
Used for the treatment of schizophrenia 4.
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- 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.
Target Actions Organism ADopamine D2 receptor antagonistHumans ADopamine D3 receptor antagonistHumans A5-hydroxytryptamine receptor 2A antagonistHumans - 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.
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- 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.
- Adverse Effects
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- Toxicity
Oral LD50 of >500 mg/kg in mice 5.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Blonanserin is combined with 1,2-Benzodiazepine. Abacavir Abacavir may decrease the excretion rate of Blonanserin which could result in a higher serum level. Abametapir The serum concentration of Blonanserin can be increased when it is combined with Abametapir. Aceclofenac Aceclofenac may decrease the excretion rate of Blonanserin which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Blonanserin which could result in a higher serum level. - Food Interactions
- Not Available
Categories
- Drug Categories
- Antidepressive Agents
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Central Nervous System Depressants
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs that are Mainly Renally Excreted
- Neurotoxic agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Chemical TaxonomyProvided by Classyfire
- 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 / Amine / Aminopyridine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Benzenoid / Dialkylarylamine / Fluorobenzene show 16 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- AQ316B4F8C
- CAS number
- 132810-10-7
- 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
References
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Blonanserin Approval Announcement [Link]
- ChemIDPlus: Blonanserin [Link]
- External Links
- KEGG Drug
- D01176
- PubChem Compound
- 125564
- PubChem Substance
- 310265129
- ChemSpider
- 111697
- BindingDB
- 50160807
- ChEBI
- 31296
- ChEMBL
- CHEMBL178803
- ZINC
- ZINC000000597434
- Wikipedia
- Blonanserin
- MSDS
- Download (42.3 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Recruiting Treatment Blonanserin / Cognition Function / First Episode Schizophrenia / Social Functioning 1 3 Completed Treatment Schizophrenia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 5.266 MSDS - Predicted Properties
Property Value Source Water Solubility 0.0359 mg/mL ALOGPS logP 5.76 ALOGPS logP 5.67 Chemaxon logS -4 ALOGPS pKa (Strongest Basic) 7.97 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 19.37 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 111.05 m3·mol-1 Chemaxon Polarizability 42.8 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 196.41666 predictedDeepCCS 1.0 (2019) [M+H]+ 198.96696 predictedDeepCCS 1.0 (2019) [M+Na]+ 207.00261 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Drug created at October 22, 2015 20:10 / Updated at February 21, 2021 18:52