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Blonanserin(AD-5423)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Blonanserin(AD-5423)图片
CAS NO:132810-10-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)367.5
FormulaC23H30FN3
CAS No.132810-10-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: N/A
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine.

InChi Key: XVGOZDAJGBALKS-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H30FN3/c1-2-26-13-15-27(16-14-26)23-17-21(18-9-11-19(24)12-10-18)20-7-5-3-4-6-8-22(20)25-23/h9-12,17H,2-8,13-16H2,1H3

SMILES Code: FC1=CC=C(C2=C(CCCCCC3)C3=NC(N4CCN(CC)CC4)=C2)C=C1

SynonymsAD 5423; AD-5423; AD5423;
实验参考方法
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.

In VivoBlonanserin, 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 modelRats
Formulation & Dosage1 mg/kg, but not 0.3 mg/kg
References

Eur J Pharmacol. 2011 Feb 25;653(1-3):47-57; Behav Brain Res. 2013 Jun 15;247:158-64.