Vabicaserin (SCA-136) is a potent, selective 5-HT2C receptor full agonist with EC50 of 8 nM, Emax 100%.
Vabicaserin displaced (125)I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT(2C) receptor sites in CHO cell membranes with Ki of 3 nM, >50-fold selective over a number of serotonergic, noradrenergic, and dopaminergic receptors.
Vabicaserin is a potent and full agonist in stimulating 5-HT(2C) receptor-coupled calcium mobilization and exhibited 5-HT(2A) receptor antagonism and 5-HT(2B) antagonist or partial agonist activity in transfected cells, depending on the level of receptor expression.
