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Discovery of orally available 8-aza-5-thiaProstaglandin E1 analogs as highly selective EP4 agonists.
Chem Pharm Bull (Tokyo)
March 2012
Minase Research Institute, Ono Pharmaceutical Co., Ltd., Mishima, Osaka 618–8585, Japan.
Analogs 8-aza-16-aryl prostaglandin E(1) (PGE(1)) and 8-aza-5-thia-16-arylPGE(1) were synthesized and evaluated with respect to their subtype receptor affinity and EP4 agonist activity for the purposes of identifying subtype-selective EP4 agonists that demonstrate oral efficacy. Using an inhibition assay of lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α production in rats, representative compounds were evaluated for their pharmacokinetic profiles and in vivo efficacy. Structure-activity relationships (SARs) were characterized and presented.
View Article and Find Full Text PDFDiscovery of an 8-aza-5-thiaProstaglandin E1 analog as a highly selective EP4 receptor agonist.
Chem Pharm Bull (Tokyo)
March 2012
Minase Research Institute, Ono Pharmaceutical Co., Ltd., Mishima, Osaka 618–8585, Japan.
For the purpose of discovering an orally available EP4 subtype-selective agonist, a series of 8-aza prostaglandin E(1) (PGE(1)) analogs were synthesized and evaluated for their affinity for PGE(2) receptor subtypes. Additionally, the structure-activity relationships of these compounds were studied. Among the tested compounds, the 8-aza PGE(1) analog 6 and 8-aza-5-thiaPGE(1) analog 12 had highly potent EP4 receptor affinity, good functional activity, and excellent subtype-selectivity.
View Article and Find Full Text PDFThe effect of a synthetic 7-thiaprostaglandin E1 derivative, TEI-6122, on monocyte chemoattractant protein-1 induced chemotaxis in THP-1 cells.
Br J Pharmacol
October 1995
Pharmaceutical Discovery Research Laboratories, Teijin Institute for Biomedical Research, Tokyo, Japan.
1 The ability of various prostaglandins (PGs) to inhibit monocyte chemotaxis induced by monocyte chemoattractant protein-1 (MCP-1) was investigated with a human monocytic leukaemia cell line, THP-1. Moreover, to investigate the mechanism of the inhibitory action of PGs the involvement of either intracellular adenosine 3': 5'-cyclic monosphosphate (cyclic AMP) accumulation or intracellular Ca2+ mobilization was studied. 2 TEI-6122, a synthetic 7-thia-PGE1 derivative, inhibited chemotaxis of THP-1 cells induced by MCP-1 with an IC50 of 1.
View Article and Find Full Text PDFIn-vivo and in-vitro hepatoprotective effect of 4-thia-prostaglandin E1 and 7-fluoroprostacyclin in rats.
J Pharm Pharmacol
May 1990
Institute for Second Biomedical Research, Teijin Ltd, Tokyo, Japan.
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