Competitive inhibition of magnesium-induced [3H]N- (1-[thienyl] cyclohexyl) piperidine binding by arcaine: evidence for a shared spermidine-magnesium binding site
Sacaan, A.I.; Johnson, K.M.
Molecular Pharmacology 38(5): 705-710
1990
ISSN/ISBN: 0026-895X PMID: 1978243 Document Number: 352068
The polyamine competitive antagonist arcaine (1,4-diguanidino-butane) produced complete inhibition of basal TCP binding, whereas glutamate and glycine have different sites of action. This is further supported by the additive effect of spermidine when tested in the presence of maximal concentrations of glutamate and glycine. On the other hand, spermidine and magnesium were not additive and, in fact, magnesium was able to block the effects of spermidine under certain conditions. The possibility that magnesium is a partial agonist at the polyamine site is discussed.