User:RelentlessRecusant/LY165163

LY165163, otherwise known as PPAP (p-Aminophenethyl-m-trifluoromethylphenyl piperazine) or LY 165,163, IUPAC name 4-[2-[4-[3-(Trifluoromethyl)phenyl]-1-piperazinyl]ethyl]benzeneamine, is a small-molecule chemical inhibitor of human and rat dopamine receptors 2 (D2) and 3 (D3) and is a chemical agonist of serotonin receptor 1A (5-HT1A).

It was extensively characterized by Milan et. al in 1995 at the Institut de Recherches Servier at Croissy-sur-Seine, France.

PPAP has been previously shown in 2007 as a highly potent and specific inhibitor of neural stem cell (NSC) and neurosphere proliferation and survival, with a 702-fold selectivity of neurosphere cultures over astrocyte cultures, and having an EC50 = 31 nM in inhibition of neurosphere diameter, inducing caspase-3 and caspase-7 within 48 hours of compound addition to neurospheres, mediating caspase-mediated apoptosis. It has significant clinical utility in that it strongly inhibits proliferation of Ptch1+/- CD133+ neurospheres, that is, adult neural cancer stem cells shown to cause brain cancer in the adult human, with an EC50 = 169 nM, compared to cyclopamine, which in this model possesses an EC50 = 1 μM.