Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

AG-D-49351 2-[9-[(4- chlorophenyl)methyl]-6- fluoro-1,2...

Synonyms: ACMC-20mq7h, CTK0H9261, PDSP1_000234, PDSP2_000233, AC1L2W6T, ...

Masuda, A. et al., Mayeux, P.R. et al., Mayeux, P.R. et al., Ueda, N. et al.

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High impact information on L657925

4. In contrast, the affinity of the TXA2/PGH2 receptor antagonists I-PTA-OH, SQ29548, and L657925 were either decreased or unchanged at pH 6.0 compared to 7 [1].
The effect of PAF was selectively blocked by PAF receptor antagonist BN50730, but not by TXA2 receptor antagonist L657925 [2].
Based on their IC50 values, the rank orders were I-BOP less than L657925 less than ONO11113 less than or equal to SQ29548 less than PTA-TPO less than PTA-NO less than or equal to L657926 less than or equal to I-PTA-OH less than PTA-OH[2] = meta-I-PTA-PO less than or equal to ONO11120[2] = ONO11120[1] less than PTA-OH[1] in rat platelets [3].
I-PTA-OH, L657925 and L657926 antagonized this response to U46619 with IC50 values similar in rank potency to that seen in the binding studies.(ABSTRACT TRUNCATED AT 250 WORDS)[4]

References

Differential effect of pH on thromboxane A2/prostaglandin H2 receptor agonist and antagonist binding in human platelets. Mayeux, P.R., Morinelli, T.A., Williams, T.C., Hazard, E.S., Mais, D.E., Oatis, J.E., Baron, D.A., Halushka, P.V. J. Biol. Chem. (1991) [Pubmed]
Receptor-mediated increase in cytosolic calcium in LLC-PK1 cells by platelet activating factor and thromboxane A2. Ueda, N., Mayeux, P.R., Walker, P.D., Shah, S.V. Kidney Int. (1991) [Pubmed]
Platelet and vascular thromboxane A2/prostaglandin H2 receptors. Evidence for different subclasses in the rat. Masuda, A., Mais, D.E., Oatis, J.E., Halushka, P.V. Biochem. Pharmacol. (1991) [Pubmed]
Human erythroleukemia cells express functional thromboxane A2/prostaglandin H2 receptors. Mayeux, P.R., Mais, D.E., Carr, C., Halushka, P.V. J. Pharmacol. Exp. Ther. (1989) [Pubmed]

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