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Suramin ‐ a powerful inhibitor of neural ecto‐diadenosine polyphosphate hydrolase
Author(s) -
Mateo Jesus,
Rotllán Pedro,
MirasPortugal M. Teresa
Publication year - 1996
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1996.tb15668.x
Subject(s) - suramin , polyphosphate , chemistry , neurotransmission , biochemistry , receptor , pharmacology , biology , phosphate
The neural ecto‐diadenosine polyphosphate hydrolase (ecto‐Ap n Aase) from plasma membranes of Torpedo synaptic terminals is inhibited by suramin. This study was carried out by discontinuous h.p.l.c. and continuous fluorometric methods. The concentration‐dependence studies showed a non‐competitive mechanism for suramin in the Dixon plot, with a K i value of 1.79 ± 0.03 μ m with respect to ɛ‐(Ap 3 A) as the substrate and 1.69 ± 0.05 μ m and 1.86 ± 0.06 μ m for ɛ‐(Ap 4 A) and ɛ‐(Ap 5 A) respectively. These results indicate that suramin could be a base compound inhibiting ecto‐Ap n Aase and providing an alternative way of studying the pharmacology of diadenosine polyphosphate receptors.