Newly synthesized analogues of the spider toxin block the crustacean glutamate receptor.
Effects of synthetic compounds similar to the structure of a spider toxin were studied on the glutamate receptors in crustacean neuromuscular synapses. Two kinds of analogues, 2,4-dihydroxyphenylacetyl-asparaginyl cadaverine (C-1) and 2,4-dihydroxyphenylacetyl-asparaginyl spermine (C-2), suppressed the excitatory postsynaptic potentials in a manner similar to natural spider toxin (JSTX). The dose-response relationship showed that the relative potency of the compounds is C-1 less than C-2 less than JSTX. While the effect of JSTX was irreversible, those of C-1 and C-2 were reversible. These synthetic compounds may serve as important tools in studying the structure and function of glutamate receptors.
Shudo
K
K
Department of Organic Chemistry, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Endo
Y
Y
Hashimoto
Y
Y
Aramaki
Y
Y
Nakajima
T
T
Kawai
N
N
D000818:Animals; D001180:Arthropod Venoms / Q000494:pharmacology*; D001216:Asparagine / Q000031:analogs & derivatives* / Q000494:pharmacology; D002103:Cadaverine / Q000031:analogs & derivatives* / Q000494:pharmacology; D003959:Diamines; D005071:Evoked Potentials / Q000187:drug effects; D005971:Glutamates / Q000502:physiology*; D008121:Nephropidae; D009469:Neuromuscular Junction / Q000187:drug effects / Q000502:physiology*; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000502:physiology*; D013096:Spermine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013111:Spider Venoms / Q000494:pharmacology*
C054638:2,4-dihydroxyphenylacetylasparaginyl spermine; D001180:Arthropod Venoms; D003959:Diamines; D005971:Glutamates; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter; D013111:Spider Venoms; C054639:2,4-dihydroxyphenylacetylasparaginyl cadaverine; D013096:Spermine; D001216:Asparagine; D002103:Cadaverine