1. Inhibition of LPS-induced TNFα production in human monocytes by adenosine (A2) receptor selective agonists
- Author
-
K.M. Esser, U. Prabhakar, D. Lipshlitz, and D.P. Brooks
- Subjects
Lipopolysaccharides ,Agonist ,medicine.medical_specialty ,medicine.drug_class ,medicine.medical_treatment ,Immunology ,Biology ,Monocytes ,chemistry.chemical_compound ,Internal medicine ,Purinergic P1 Receptor Agonists ,medicine ,Humans ,Receptor ,Cells, Cultured ,Pharmacology ,Tumor Necrosis Factor-alpha ,Monocyte ,Xanthine ,Adenosine ,Endocrinology ,Cytokine ,medicine.anatomical_structure ,Purinergic P1 Receptor Antagonists ,chemistry ,Xanthines ,DMPX ,Theobromine ,Tumor necrosis factor alpha ,Immunosuppressive Agents ,medicine.drug - Abstract
We examined the effects of adenosine A 1 and A 2 receptor agonists on LPS-stimulated TNFα production by human monocytes isolated from peripheral blood. We have demonstrated that CGS-21680, a highly selective A 2 agonist inhibited production of TNFα at the protein level by 75% whereas the A 1 selective agonist N 6 reduced TNFα production by only 25%. The action of CGS-21680 was mediated via the A 2 receptors since its effect on TNF production was blocked by 3,7-dimethyl-l-propargylxanthine (DMPX) but not by xanthine amine cogener (XAC), antagonists selective for the A 2 and A 1 receptors, respectively. Thus intervention with A 2 -selective agonists or compounds that can elevate endogenously released adenosine may be beneficial in TNFα-mediated diseases.
- Published
- 1995