Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors
| Autor: | Kenneth A. Jacobson, Ariel S. Gross, Zhan-Guo Gao |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2004 |
| Předmět: |
Receptor
Adenosine A2A Class C GPCR CHO Cells Pharmacology Astrocytoma Kidney Binding Competitive General Biochemistry Genetics and Molecular Biology Article Adenosine A1 receptor Radioligand Assay Receptors Purinergic P2Y1 Allosteric Regulation Cricetinae Thiadiazoles Animals Humans General Pharmacology Toxicology and Pharmaceutics Receptor Cells Cultured G protein-coupled receptor Chemistry Brain Neoplasms Receptor Adenosine A1 Receptors Purinergic P2 Receptor Adenosine A3 General Medicine Purinergic signalling Adenosine A3 receptor Adenosine receptor Rats Kinetics Thiazoles Adenosine A2B receptor |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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