Uptake and release of kyotorphin in rat brain synaptosomes

Uptake and release of kyotorphin (Tyr-Arg) in rat brain synaptosomes were studied. Synthetic kyotorphin was taken up into crude synaptosomes (P2), in a temperature-dependent manner. The Km and Vmax of the uptake were 1.31 +/- 0.12 X 10(-4) M and 5.9 +/- 0.5 pmol/mg protein/min, respectively. Metabolic inhibitors such as dinitrophenol and iodoacetamide and ouabain which is known as an inhibitor of Na+ dependent uptake mechanism significantly inhibited the uptake. When the synaptosomes previously preloaded with synthetic kyotorphin at 10(-4)M were exposed to high K+ medium, kyotorphin was released in a Ca2+-dependent manner. These findings support the view that kyotorphin plays a role as neurotransmitter/neuroregulator.