Neuroanatomical distribution and binding properties of saxitoxin sites in the rat and turtle CNS.

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Since saxitoxin (STX) binds to voltage-sensitive sodium channels and blocks their function, it has been widely used in the study of these channels. There is, however, limited information on STX binding properties and the neuroanatomical distribution of the Na+ channel as a function of brain region in the rat and in lower vertebrates such as the turtle. In the present study, we used a broad range of 3H-STX concentration (up to 64 nM) to examine saturation profiles and density distribution in both adult rat and turtle brains. We found that (1) STX sites do not vary greatly in affinity (most Kds = 2 to 5 nM) in various regions of the adult rat brain; (2) STX binding distribution was very heterogeneous in the rat with much higher density in the cortex, hippocampus, amygdala, and cerebellum than in the brainstem and spinal cord; (3) STX sites are mostly localized in layers made mostly of neurons with low density in white matter; and (4) turtle brain STX sites had similar binding properties, but its brain had much fewer STX sites than the rat, especially in the cerebellum and rostral areas such as the cortex. We conclude that (a) adult brain sodium channels have similar STX binding affinity in spite of the existence of multiple sodium channel subtypes; (b) the brainstem is very different from rostral brain areas in channel density; and (c) the turtle brain has a much lower sodium channel density than the rat brain.