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Blonanserin
Systematic (IUPAC) name
2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
Identifiers
CAS number 132810-10-7
ATC code none
PubChem 125564
ChemSpider 111697
Chemical data
Formula C23H30FN3 
Mol. mass 367.50 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status Prescription only
Routes Oral

Blonanserin (Lonasen) is a relatively new atypical antipsychotic commercialized by Dainippon Sumitomo Pharma in Japan and Korea for the treatment of schizophrenia.[1][2][3] Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms and excessive sedation and hypotension.[3]

Blonanserin acts as a mixed 5-HT2 (Ki = 3.98 nM) and D2 receptor (Ki = 14.8 nM) antagonist.[4] It also exerts some blockade of α1-adrenergic receptors (Ki = 56.3 nM) and has low affinity for the sigma receptor (IC50 = 286 nM).[4] Blonanserin lacks significant affinity for numerous other sites including 5-HT1, 5-HT3, D1, α2-adrenergic, β-adrenergic, H1, mACh, and the monoamine transporters.[4]

See also

References

  1. ^ Deeks ED, Keating GM (January 2010). "Blonanserin: a review of its use in the management of schizophrenia". CNS Drugs 24 (1): 65–84. doi:10.2165/11202620-000000000-00000. PMID 20030420. http://content.wkhealth.com/linkback/openurl?issn=1172-7047&volume=24&issue=1&spage=65. 
  2. ^ Garcia E, Robert M, Peris F, Nakamura H, Sato N, Terazawa Y (2009). "The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study". CNS Drugs 23 (7): 615–25. PMID 19552488. http://content.wkhealth.com/linkback/openurl?issn=1172-7047&volume=23&issue=7&spage=615. 
  3. ^ a b Heading CE (November 1998). "AD-5423 (Dainippon Pharmaceutical Co Ltd)". IDrugs : the Investigational Drugs Journal 1 (7): 813–7. PMID 18465651. 
  4. ^ a b c Oka M, Noda Y, Ochi Y, et al. (January 1993). "Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties". The Journal of Pharmacology and Experimental Therapeutics 264 (1): 158–65. PMID 8093723. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8093723. 
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