M. Miyashita, SYNTHETIC STUDIES ON NEPHILATOXINS, NEW N EUROTOXINS OF JORO SPIDER (NEPHILA-CLAVATA), Yuki Gosei Kagaku Kyokaishi, 54(10), 1996, pp. 846-858
Synthetic studies on nephilatoxins which has been carried out in the a
uthor's group is reviewed. Nephilatoxins (NPTX-1 similar to 12) isolat
ed from Joro Spider (Nephila clavata) have been demonstrated to be pot
ent blockers of glutaminergic neurotransmission as well as other spide
r toxins and are emerging as unique tools for understanding excitatory
amino acid neurotransmission. In this report chemical synthesis of sp
ider toxins involving synthetic strategy and total synthesis of NPTX-7
similar to 12 is described in which three azide intermediates were de
signed and employed as key compounds for construction of the character
istic polyamine chains of the toxins. In addition new results of biolo
gical activities obtained by using synthetic nephilatoxins (NPTX-7 sim
ilar to 12) and their congeners incorporating a D-amino acid are also
described.