INHIBITION OF HIV-INFECTION OF H9 CELLS BY CHLORPROMAZINE DERIVATIVES

The binding between the HIV surface protein. gp120, and the CD4 corece ptor is known to be initiated by electrostatic interactions. Because o f the ability of chlorpromazine to interact with proteins by charge tr ansfer, we tested several derivatives for their ability to block bindi ng of HIV to CD4(+) cells. We have shown that 7,8-dioxo-chlorpromazine blocks binding of fluorescein isothiocyanate-labeled anti-Leu3a and r gp120 to peripheral human blood T4 cells and blocks syncytia formation between gp120- and CD4-expressing cells. We also found that 7,8-dioxo -chlorpromazine blocks HIV infectivity of H9 cells and acts synergisti cally with zidovudine.