Description
SCH-202676 (70375-43-8) is a reversible inhibitor of both agonist and antagonist binding to G protein-coupled receptors (GPCRs).1 IC50‘s = 0.1-1.7 μM for nine GPCRs.1 Modification of GPCRs is accomplished via sulfhydryl modification.2,3
Uses
SCH-202676 hydrobromide is a modulator that inhibits binding to G protein-coupled receptors.
Biological Activity
Sulphydryl-reactive compound that inhibits agonist and antagonist binding to G-protein-coupled receptors. Inhibits a variety of GPCRs including adenosine, opioid, muscarinic, adrenergic and dopaminergic receptors (IC 50 values are 0.1-1.8 μ M).
References
1) Fawzi et al. (2001), SCH-202676: an allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors; Mol.Pharmacol. 59 30
2) Lewandowicz et al. (2006), The allosteric modulator SCH-202676 disrupts G protein-coupled receptor function via sulphydryl-sensitive mechanisms; Br. J. Pharmacol. 147 422
3) Goblyos et al. (2005), Synthesis and biological evaluation of a new series of 2,3,5-substituted[1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action; J. Med. Chem., 48 1145
