Blonanserin

Catalog No.S2112 Synonyms: AD 5423

Blonanserin  Chemical Structure

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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Biological Activity

Description Blonanserin is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.
Targets
5-HT2 [1] dopamine D2 receptor [1]
3.98 nM(Ki) 14.8 nM(Ki)
In vitro

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. [1] Blonanserin increases the efflux of cortical DA and its metabolites, homovanillic acid and 3,4-dihydroxyphenylacetic acid. [2] 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). [3] Blonanserin, a novel atypical antipsychotic agent with dopamine D(2)/serotonin 5-HT(2A) antagonistic properties, displays good brain distribution. [4]

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. [5]

Protocol

Solubility (25°C)

In vitro DMF 30 mg/mL warmed (81.63 mM)
DMSO Insoluble
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 367.5
Formula

C23H30FN3

CAS No. 132810-10-7
Storage powder
Synonyms AD 5423

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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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5-HT Receptor Signaling Pathway Map

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