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Beschreibung

A suramin analog that acts as a selective G-protein antagonist for &alpha,-subunits of the Go/Gi group (EC50 ~300 nM). Suppresses GTP&gamma,S binding to recombinant G-protein &alpha,-subunits. Acts by inhibiting the formation of the agonist-specific ternary complex (agonist/receptor/G-protein). NF023 does not interfere with the interaction between &alpha,-subunits &beta,&gamma,-dimer but competes with the effector binding site. Also a P2X receptor antagonist (IC50=0.24 microM for P2X1, 8.5 microM for P2X3 receptor in rat muscle)., A suramin analog that acts as a selective and direct G-protein antagonist for &alpha,-subunits of the Go/Gi group (EC50 ~ 300 nM). Suppresses GTP&gamma,S binding to recombinant G-protein &alpha,-subunits. Acts by inhibiting the formation of the agonist-specific ternary complex (agonist/receptor/G-protein). NF023 does not interfere with the interaction between &alpha,-subunits and &beta,&gamma,-dimer but competes with the effector binding site. Also a P2X receptor antagonist (IC50 = 240 nM for P2X1, 8.5 microM for P2X3 receptor in rat muscle). Causes a concentration dependent inhibition of excitatory junction potentials (IC50 = 4.8 pM).