Catalog No.S2112 Synonyms: AD 5423
Molecular Weight(MW): 367.5
Blonanserin is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.
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|Description||Blonanserin is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.|
Blonanserin transiently increases neuronal firing in locus coeruleus and ventral tegmental area but not in dorsal raphe nucleus or mediodorsal thalamic nucleus, whereas Risperidone increases the firing in locus coeruleus, ventral tegmental area and dorsal raphe nucleus but not in mediodorsal thalamic nucleus of rats. Blonanserin persistently increases frontal extracellular levels of norepinephrine and dopamine but not serotonin, GABA or glutamate, whereas Risperidone persistently increases those of norepinephrine, dopamine and serotonin but not GABA or glutamate.  Blonanserin increases the efflux of cortical DA and its metabolites, homovanillic acid and 3,4-dihydroxyphenylacetic acid.  Blonanserin shows the most potent binding affinity for human D3 receptors among the tested atypical antipsychotics (risperidone, olanzapine and aripiprazole). Blonanserin acts as a potent full antagonist for human D3 receptors. Blonanserin blocks the binding of [(3)H]-(+)-PHNO, a D2/D3 receptor radiotracer, both in the D2 receptor-rich region (striatum) and the D3 receptor-rich region (cerebellum lobes 9 and 10).  Blonanserin, a novel atypical antipsychotic agent with dopamine D(2)/serotonin 5-HT(2A) antagonistic properties, displays good brain distribution. 
|In vivo||Blonanserin, 1 mg/kg, but not 0.3 mg/kg, improves the PCP-induced NOR deficit in rats. Blonanserin significantly reverses the NOR deficit without diminishing activity during the acquisition or retention periods in rats. |
-  Ohoyama K, et al. Eur J Pharmacol,?011, 653(1-3), 47-57.
-  Huang M, et al. J Neurochem,?014, 128(6), 938-949.
-  Baba S, et al. J Pharmacol Sci,?015, 127(3), 326-331.
|In vitro||DMF||30 mg/mL warmed (81.63 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01516424||Completed||Schizophrenia||Sumitomo Pharmaceutical (Suzhou) Co., Ltd.||February 2012||Phase 3|
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