Agonists bind with higher affinity to G protein-coupled heptahelical receptors than to uncoupled receptors. Recombinant A1 and A3 adenosine receptors couple well to Gi/o, but recombinant human A2A adenosine receptors (hA2AAR) couple poorly to Gs and bind agonists with Ki values in binding assays that are much higher than ED50 values for functional responses such as coronary dilation and inhibit...

Agonists bind with higher affinity to G protein-coupled heptahelical receptors than to uncoupled receptors. Recombinant A1 and A3 adenosine receptors couple well to Gi/o, but recombinant human A2A adenosine receptors (hA2AAR) couple poorly to Gs and bind agonists with Ki values in binding assays that are much higher than ED50 values for functional responses such as coronary dilation and inhibit...

Under normoxic conditions, macrophages from C57BL mice produce low levels of vascular endothelial growth factor (VEGF). Hypoxia stimulates VEGF expression by approximately 500%; interferon-gamma (IFN-gamma) with endotoxin [lipopolysaccharide (LPS)] also stimulates VEGF expression by approximately 50 to 150% in an inducible nitric oxide synthase (iNOS)-dependent manner. Treatment of normoxic mac...

The A(2A) adenosine receptor (A(2A)AR) mediates anti-inflammatory actions of adenosine in a variety of cell types. LPS (lipopolysaccharide) was reported to induce a small (<2-fold) increase in the expression of A(2A)AR mRNA in human monocytes and monocytic cell lines. We investigated the effects of LPS on the expression of adenosine receptor mRNAs in primary mouse IPMPhi (intraperitoneal macrop...

Bacterial lipopolysaccharide (LPS) activates the immune system and promotes inflammation via Toll-like receptor (TLR) 4, which regulates the synthesis and release of tumor necrosis factor (TNF)and other inflammatory cytokines. Previous studies have shown that the nucleoside adenosine suppresses LPS-stimulated TNFrelease in human UB939 macrophages by activating an adenosine A3 receptor (A3AR) su...

*Morino, T; +*Ogata, T; *Horiuchi, H; *Hamamoto, Y; *Hino, M; *Yamamoto, H +*Department of Orthopaedic Surgery, Ehime University, Shitsukawa, Tohon city, Ehime 791-0295, JAPAN [email protected] Introduction After spinal cord injury, severe sensory disturbances occur, accompanied by motor deficiencies. Some patients with spinal cord injury complain of feeling several kinds of pain sensations...

Purpose: Regulatory T cell (Treg) frequency and activity are increased in cancer patients and play a major role in tumor escape. Although disease progression is favored by the presence of Treg, mechanisms used by Treg to suppress antitumor immunity are unknown. The ectonucleotidases CD39 and CD73 are expressed in Treg and convert ATP into immunosuppressive adenosine. In this study, the involvem...

Human immunodeficiency virus dementia (HIV-D) is a nonfocal central nervous system manifestation characterized by cognitive, behavioral, and motor abnormalities. The pathophysiology of neuronal damage in HIV-D includes a direct toxic effect of viral proteins on neuronal cells and an indirect effect caused by the release of inflammatory mediators and neurotoxins by activated macrophages/microgli...

Rat pheochromocytoma (PC12) cells characteristically undergo differentiation when cultured with nerve growth factor (NGF). Here we show that NGF dramatically increased the adenylyl cyclase-activating property of forskolin in PC12 cells. This effect of NGF was well maintained even when NGF was removed after 4 days, even though the morphological features of neuronal differentiation were rapidly l...