Using Fura-2AM microfluorimetry we have shown for the first time that sigma-1 receptor antagonist neuroleptic chlorpromazine – significantly inhibits glutoxim- and molixan-induced Ca²⁺ responses and Ca²⁺ responses, induced by endoplasmic reticulum Са²⁺-ATPase inhibitors thapsigargin and cyclopiazonic acid, in rat peritoneal macrophages. The results suggest the involvement of sigma-1 receptors in signaling cascade induced by glutoxim or molixan and leading to intracellular Ca²⁺ concentration increase, and in the regulation of store-dependent Ca²⁺-entry, in macrophages.