Spermine modulation of specific [~3H]-gabapentin binding to the detergent-solubilized porcine cerebral cortex σ_2δ calcium channel subunit

摘要

The finding that [~3H]-gabapentin binding to the pure α_2δsubunit was stimulated by spermine indicates that the α_2δ subunit of voltage-sensitive calcium channels beasrs a modulatory spermine site. Such a spermine site has not been identified before. Spermine stimulation of [~3H]-gabapentin binding to the purified protein was reversed to inhibition after adding back dialysate. Thus the inhibitory spermine effect in membranes is also probably due to one or more modulatory sites on the α_2δ subunit.