mrs-1191 and 9-(3-hydroxy-2-phosphonomethoxypropyl)-2-6-diaminopurine

mrs-1191 has been researched along with 9-(3-hydroxy-2-phosphonomethoxypropyl)-2-6-diaminopurine* in 1 studies

Other Studies

1 other study(ies) available for mrs-1191 and 9-(3-hydroxy-2-phosphonomethoxypropyl)-2-6-diaminopurine

Article	Year
Nucleotide analogues with immunobiological properties: 9-[2-Hydroxy-3-(phosphonomethoxy)propyl]-adenine (HPMPA), -2,6-diaminopurine (HPMPDAP), and their N6-substituted derivatives. European journal of pharmacology, 2006, Jul-01, Volume: 540, Issue:1-3 Newly developed acyclic nucleoside phosphonates, derivatives of adenine and 2,6-diaminopurine bearing the 2-hydroxy-3-(phosphonomethoxy)propyl (HPMP) moiety at the N9-side chain (i.e., HPMPA and HPMPDAP, respectively) were screened for in vitro immunobiological activity, using mouse resident peritoneal macrophages and splenocytes. Both HPMPA and HPMPDAP augmented the interferon-gamma-triggered production of NO as well as expression of inducible nitric oxide synthase (iNOS) mRNA in macrophages. HPMPDAP activated secretion of tumor necrosis factor-alpha (TNF-alpha), chemokines "regulated-upon-activation, normal T cell expressed and secreted" (RANTES) and macrophage inflammatory protein-1alpha (MIP-1alpha), and marginally also secretion of interleukin-10 (IL-10) in both macrophages and splenocytes. The HPMPA, less prominently than HPMPDAP, elevated only secretion of RANTES and TNF-alpha. The compounds also activated secretion of TNF-alpha (HPMPDAP > HPMPA) in human peripheral blood mononuclear cells (PBMC). Distinct N6-substituted derivatives, i.e., N6-dimethyl-, N6-cyclopropyl-, N6-piperidin-1-yl-, N6-(2-methoxyethyl)-, N6-(2-hydroxyethyl)-, N6-allyl- and N6-2-(dimethylamino)ethyl-HPMPA/HPMPDAP as well as 6-thio and 6-hydroxy derivatives usually showed loss of the activity compared to the parent compounds. The immunomodulatory effects were found to be at least in part dependent on P1 purinoreceptors, and mediated by transcriptional factor nuclear factor-kappaB. Topics: Adenine; Animals; Caffeine; Cell Survival; Cytokines; Dihydropyridines; Dose-Response Relationship, Drug; Female; Gene Expression; Interferon-gamma; Lipopolysaccharides; Macrophages, Peritoneal; Mice; Mice, Inbred C57BL; Molecular Structure; Nitric Oxide; Nitric Oxide Synthase Type II; Nucleotides; Organophosphonates; Organophosphorus Compounds; Purinergic P1 Receptor Antagonists; Quinazolines; Receptors, Purinergic P1; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Triazoles	2006

Article

Year

Nucleotide analogues with immunobiological properties: 9-[2-Hydroxy-3-(phosphonomethoxy)propyl]-adenine (HPMPA), -2,6-diaminopurine (HPMPDAP), and their N6-substituted derivatives.

European journal of pharmacology, 2006, Jul-01, Volume: 540, Issue:1-3

Newly developed acyclic nucleoside phosphonates, derivatives of adenine and 2,6-diaminopurine bearing the 2-hydroxy-3-(phosphonomethoxy)propyl (HPMP) moiety at the N9-side chain (i.e., HPMPA and HPMPDAP, respectively) were screened for in vitro immunobiological activity, using mouse resident peritoneal macrophages and splenocytes. Both HPMPA and HPMPDAP augmented the interferon-gamma-triggered production of NO as well as expression of inducible nitric oxide synthase (iNOS) mRNA in macrophages. HPMPDAP activated secretion of tumor necrosis factor-alpha (TNF-alpha), chemokines "regulated-upon-activation, normal T cell expressed and secreted" (RANTES) and macrophage inflammatory protein-1alpha (MIP-1alpha), and marginally also secretion of interleukin-10 (IL-10) in both macrophages and splenocytes. The HPMPA, less prominently than HPMPDAP, elevated only secretion of RANTES and TNF-alpha. The compounds also activated secretion of TNF-alpha (HPMPDAP > HPMPA) in human peripheral blood mononuclear cells (PBMC). Distinct N6-substituted derivatives, i.e., N6-dimethyl-, N6-cyclopropyl-, N6-piperidin-1-yl-, N6-(2-methoxyethyl)-, N6-(2-hydroxyethyl)-, N6-allyl- and N6-2-(dimethylamino)ethyl-HPMPA/HPMPDAP as well as 6-thio and 6-hydroxy derivatives usually showed loss of the activity compared to the parent compounds. The immunomodulatory effects were found to be at least in part dependent on P1 purinoreceptors, and mediated by transcriptional factor nuclear factor-kappaB.

Topics: Adenine; Animals; Caffeine; Cell Survival; Cytokines; Dihydropyridines; Dose-Response Relationship, Drug; Female; Gene Expression; Interferon-gamma; Lipopolysaccharides; Macrophages, Peritoneal; Mice; Mice, Inbred C57BL; Molecular Structure; Nitric Oxide; Nitric Oxide Synthase Type II; Nucleotides; Organophosphonates; Organophosphorus Compounds; Purinergic P1 Receptor Antagonists; Quinazolines; Receptors, Purinergic P1; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Triazoles

2006