Vabicaserin HCl can replace the binding of 125I-(2,5-dimethoxy)phenylisopropylamine at the human 5-HT2C receptor site on the CHO cell membrane, with a Ki value of 3 nM, and its selectivity exceeds some serotonergic, noradrenergic and 50 times more dopaminergic receptors. The binding affinity to the human 5-HT2B receptor subtype was determined to be 14 nM using [3H]5HT. Vabicaserin HCl is a potent full agonist (EC50, 8 nM; Emax, 100%) in stimulating 5-HT2C receptor-coupled calcium mobilization. Depending on the receptor expression level in transfected cells, it exhibits 5-HT2A receptor antagonism and 5-HT2B antagonism or partial agonistic activity. Vabicaserin exhibits lower affinity at the 5-HT2C antagonist binding site labeled with [3H]mesulergine (22 nM). Additional binding studies have shown that Vabicaserin has affinity for the 5-HT2B and 5-HT1A receptors with Ki values of 14 nM and 112 nM, respectively [1] .
Vabicaserin HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rodents
Schizophrenia animal models
Intraperitoneal injection
3, 10, 17 mg/kg
Not specified
To evaluate the effect of Vabicaserin on dopamine neuron activity, results showed that Vabicaserin significantly decreases the number of spontaneously active mesocorticolimbic dopamine neurons without affecting nigrostriatal dopamine neurons.
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