N-(2,3-Diphenyl-1,2,4-thiadiazol-5(2H)-ylidene)methanamine hydrobromide

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).

IC 50

Adenosine A₃ receptor

References

[1] A B FAWZI. SCH-202676: An allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors.[J]. Molecular Pharmacology, 2001, 59 1: 30-37. DOI:10.1124/mol.59.1.30
[2] ANNA M LEWANDOWICZ  Jarmo T L  Jouko Vepsäläinen. The “allosteric modulator” SCH-202676 disrupts G protein-coupled receptor function via sulphydryl-sensitive mechanisms.[J]. British Journal of Pharmacology, 2006, 147 4: 422-429. DOI:10.1038/sj.bjp.0706624
[3] ANIKÓ GÖBLYÖS. 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]. Journal of Medicinal Chemistry, 2005, 48 4: 1145-1151. DOI:10.1021/jm049337s