The mitochondrial membrane permeability transition induced by Ca2+ is inhib
ited by quinine in a dose-dependent fashion. Competition experiments strong
ly suggest that quinine displaces Ca2+ bound to the inner membrane. This is
supported by experiments showing that quinine inhibits Ca2+-dependent but
not Ca2+-independent mitochondrial swelling induced by phenylarsine oxide.
As with Ca2+ chelators, quinine induces permeability transition pore closur
e preventing the contraction induced by poly(ethylene glycol) 2000 in mitoc
hondria preswollen by incubation in KSCN medium containing Ca2+ and inorgan
ic phosphate,These results suggest that quinine dislodges Ca2+ bound to the
protein site, which triggers pore opening.