1996 年 54 巻 10 号 p. 846-858
Synthetic studies on nephilatoxins which has been carried out in the author's group is reviewed. Nephilatoxins (NPTX-112) isolated from Joro Spider (Nephila clavata) have been demonstrated to be potent blockers of glutaminergic neurotransmission as well as other spider toxins and are emerging as unique tools for understanding excitatory amino acid neurotransmission. In this report chemical synthesis of spider toxins involving synthetic strategy and total synthesis of NPTX-712 is described in which three azide intermediates were designed and employed as key compounds for construction of the characteristic polyamine chains of the toxins. In addition new results of biological activities obtained by using synthetic nephilatoxins (NPTX-712) and their congeners incorporating a D-amino acid are also described.