SCH 202676 hydrobromide

SCH 202676 is a reversible inhibitor of both agonist and antagonist binding to diverse G protein-coupled receptors (GPCRs).1 It blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors.[1],[2],[3] It displays IC50 values of 0.1 to 1.8 µM for modulating ligand binding.1,2 SCH 202676 may modulate GPCRs via thiol modification.[4]

References
[1]. Fawzi, A.B., Macdonald, D., Benbow, L.L., et al. SCH-202676: An allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors. Molecular Pharmacology 59(1), 30-37 (2001).
[2]. Gao, Z.G., Kim, S.K., Ijzerman, A.P., et al. Allosteric modulation of the adenosine family of receptors. Mini Rev.Med.Chem. 5(6), 545-553 (2005).
[3]. Lanzafame, A., and Christopoulos, A. Investigation of the interaction of a putative allosteric modulator, N-(2,3-diphenyl-1,2,4-thiadiazole-5-(2H)-ylidene) methanamine hydrobromide (SCH-202676), with M1 muscarinic acetylcholine receptors. Journal of Pharmacology and Experimental Therapeutics 308(3), 830-837 (2004).
[4]. Lewandowicz, A.M., Vepsäläinen, J., and Laitinen, J.T. The 'allosteric modulator' SCH-202676 disrupts G protein-coupled receptor function via sulphydryl-sensitive mechanisms. British Journal of Pharmacology 147(4), 422-429 (2006).