product name Blonanserin
Description: Blonanserin (also known as AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, ut is used the treatment of schizophrenia. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As with many second-generation (atypical) antipsychotics, Blonanserin is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics such as haloperidol.
References: Eur J Pharmacol. 2011 Feb 25;653(1-3):47-57; Behav Brain Res. 2013 Jun 15;247:158-64.
367.5
Formula
C23H30FN3
CAS No.
132810-10-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO:
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
AD 5423
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Eur J Pharmacol. 2011 Feb 25;653(1-3):47-57; Behav Brain Res. 2013 Jun 15;247:158-64. |
