Home Neuronal Signaling 5-HT Receptor antagonist Blonanserin

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Blonanserin 5-HT Receptor antagonist

Cat.No.S2112

Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.
Blonanserin 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 367.5

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Quality Control

Batch: S211201 5%TFA]3 mg/mL]false]DMSO]Insoluble]false]Water]Insoluble]false Purity: 99.72%
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99.72

Solubility

In vitro
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5%TFA : 3 mg/mL

DMSO : Insoluble
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Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 367.5 Formula

C23H30FN3

 Storage (From the date of receipt)
CAS No. 132810-10-7 Download SDF Storage of Stock Solutions

Synonyms AD 5423 Smiles CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(C=C4)F

Mechanism of Action

Targets/IC50/Ki
5-HT2
3.98 nM(Ki)
dopamine D2 receptor
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. This compound 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. It increases the efflux of cortical DA and its metabolites, homovanillic acid and 3,4-dihydroxyphenylacetic acid. This chemical shows the most potent binding affinity for human D3 receptors among the tested atypical antipsychotics (risperidone, olanzapine and aripiprazole). It acts as a potent full antagonist for human D3 receptors. It 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). This agent, a novel atypical antipsychotic 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. This compound significantly reverses the NOR deficit without diminishing activity during the acquisition or retention periods in rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22691713/
  • [5] https://pubmed.ncbi.nlm.nih.gov/23538066/

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