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Chemical Compound Review:

AFP-07 (5Z)-5-[(1R,5S,7R,8S)-2,2- difluoro-7...

Synonyms: AFP07, AC1NSK95

Jones, R.L. et al., Chang, C.S. et al., Chow, K.B. et al.

Jones, Chan,

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High impact information on AFP-07

The possibility that the prostacyclin analogues AFP-07 and cicaprost relax saphenous vein preparations of pig, guinea-pig and rabbit by simultaneously activating prostanoid EP4 and IP (prostacyclin) receptors was investigated using the high-affinity EP4 antagonist GW 627368 [1].
For hIP, the order of potency (pEC(50)) for stimulating AC and PLC pathways was similar: AFP-07 (9.3, 8.4)>cicaprost (8.3, 6.9), iloprost (7.9, 6.8)>taprostene (7.4, 6.8)>carbacyclin (6.9, 6.6), PGE(1) (6.6, 5.1) [2].
7,7-Difluoroprostacyclin derivative, AFP-07, a highly selective and potent agonist for the prostacyclin receptor [3].
AFP-07 strongly displaced the [3H] iloprost binding to the IP receptor-expressing cell membranes, the half maximal concentration for the displacement being 3 nM, which was one order lower than that of iloprost [3].

Anatomical context of AFP-07

The results indicate that AFP-07 and cicaprost are moderately potent EP4 agonists on pig saphenous vein, but much weaker EP4 agonists on guinea-pig saphenous vein [1].

References

Investigation of the agonist activity of prostacyclin analogues on prostanoid EP4 receptors using GW 627368 and taprostene: evidence for species differences. Jones, R.L., Chan, K.M. Prostaglandins Leukot. Essent. Fatty Acids (2005) [Pubmed]
Agonists can discriminate between cloned human and mouse prostacyclin receptors. Chow, K.B., Jones, R.L., Wise, H. Prostaglandins Leukot. Essent. Fatty Acids (2004) [Pubmed]
7,7-Difluoroprostacyclin derivative, AFP-07, a highly selective and potent agonist for the prostacyclin receptor. Chang, C.S., Negishi, M., Nakano, T., Morizawa, Y., Matsumura, Y., Ichikawa, A. Prostaglandins (1997) [Pubmed]

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