SCH 202676 hydrobromide - CAS 265980-25-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
SCH 202676 hydrobromide is a reversible inhibitor of agonist and antagonist binding to G-protein-coupled receptors. It inhibits a variety of GPCRs including adenosine, opioid, muscarinic, adrenergic and dopaminergic receptors (IC50 = 0.1-1.8 μM).
Brife Description:
inhibitor of GPCR agonist and antagonist
≥99% by HPLC
Related CAS:
70375-43-8 (free base)
SCH 202676 hydrobromide; SCH202676 hydrobromide; SCH-202676 hydrobromide; N-(2,3-Diphenyl-1,2,4-thiadiazol-5(2H)-ylidene)methanamine hydrobromide
Melting Point:
>223°C (dec.)
Canonical SMILES:
1.Increased Neuronal Depolarization Evoked by Autoantibodies in Diabetic Obstructive Sleep Apnea: Role for Inflammatory Protease(s) in Generation of Neurotoxic Immunoglobulin Fragment.
Zimering MB;Pan Z J Endocrinol Diabetes. 2017;4(1). doi: 10.15226/2374-6890/4/1/00168. Epub 2017 Jan 22.
11 Aim: ;Obstructive sleep apnea increases in diabetes and morbid obesity. We tested a hypothesis that circulating autoantibodies in adult type 2 diabetes which increase in association with morbid obesity are capable of causing long-lasting neuronal depolarization and altered calcium release in mouse atrial cardiomyocytes.;12 Methods: ;Protein-A eluates from plasma of 14 diabetic obstructive sleep apnea patients and 17 age-matched diabetic patients without sleep apnea were tested for effects on depolarization and neurite out growth in N2a mouse neuroblastoma cells. The mechanism of autoantibody-mediated neurite outgrowth inhibition was investigated in co-incubation experiments of diabetic obstructive sleep apnea autoantibodies with specific antagonists of G-protein coupled receptors or the RhoA/Rho kinase signaling pathway. Following long-term storage of the protein-A eluates (to allow spontaneous proteolysis and IgG subunit dissociation), plasma autoantibodies from diabetic obstructive sleep apnea, cancer or control patients were compared for enhancement of inhibitory effects on endothelial cell survival. Size exclusion chromatography performed (in the presence or absence of a specific membrane type 1-matrix metalloproteinase inhibitor) was used to characterize the IgG autoantibody subunit(s) or fragments associated with peak neurotoxicity in diabetic obstructive sleep apnea.
2.Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors.
Gao ZG;Gross AS;Jacobson KA Life Sci. 2004 May 7;74(25):3173-80.
The G protein-coupled receptor allosteric modulator SCH-202676 (N-(2,3-diphenyl-1,2,4-thiadiazol-5-(2H)-ylidene)methanamine), which affects a wide range of structurally unrelated G protein-coupled receptors, has highly divergent effects on purine receptors. SCH-202676 inhibited radioligand binding to human adenosine A(1), A(2A), and A(3) receptors (IC(50) = 0.5-0.8 microM) and affected dissociation kinetics, but at the human P2Y(1) nucleotide receptor it had no effect. SCH-202676 (10 microM) selectively accelerated agonist dissociation at adenosine A(3) receptors and either slowed (adenosine A(1) receptors) or accelerated (adenosine A(2A) receptors) antagonist dissociation. Thus, SCH-202676 differentially modulated A(1), A(2A), and A(3) receptors as well as agonist- and antagonist-occupied receptors.
3.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.
Göblyös A;de Vries H;Brussee J;Ijzerman AP J Med Chem. 2005 Feb 24;48(4):1145-51.
We synthesized two series (7a-i and 8a-i) of 2,3,5-substituted [1,2,4]-thiadiazole analogues of SCH-202676 (7a, 2,3-diphenyl-5-N-methylimino-2H-[1,2,4]-thiadiazole) with emphasis on the N-imino substituent. Compounds 7a-g,i and 8a-g at a final concentration of 1 microM significantly inhibited [(3)H]CCPA (2-chloro-N(6)- cyclopentyladenosine) agonist binding to human A(1) adenosine receptors. At the same concentration, all compounds appeared to increase [(3)H]DPCPX (1,3-dipropyl-8-cyclopentylxanthine) antagonist binding. Compound 7a and LUF5855 (7g) were selected for further characterization and studied in both equilibrium and kinetic radioligand binding experiments. The results suggest a nonstoichiometric interaction with the receptor. Further bioanalytical procedures (HPLC and MS) provided proof for an unusual receptor interaction in which 7a and 7g upon incubation were transformed into their corresponding thioureas 5a and 5g. We suggest that the thiadiazoles are sulfhydryl modifying agents rather than allosteric modulators, as they appear to reversibly modify the sulfhydryl groups of cysteine residues in cell membrane preparations.
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CAS 265980-25-4 SCH 202676 hydrobromide

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