16(R)-AFP 07 (free acid)

Description

Prostaglandin I₂ is an unstable prostanoid which, through the ‘I prostanoid’ (IP) receptor, inhibits platelet aggregation and promotes vasodilatation in pulmonary vascular beds. AFP 07 is a 7,7-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (K_i = 0.561 nM).¹ AFP 07 shows weaker affinity for EP receptors, with K_i values > 100 nM for EP_1-3 and > 10 nM for EP₄.^1,2 16(R)-AFP 07 is an epimer of AFP 07. Its biological properties, particularly through the IP and EP receptors, remain to be evaluated.

References

1. Chang, C.s., Negishi, M., Nakano, T., et al. 7,7-Difluoroprostacyclin derivative, AFP-07, a highly selective and potent agonist for the prostacyclin receptor Prostaglandins 53(2),83-90(1997).
2. Jones, R.L., and Chan, K. Distinction between relaxations induced via prostanoid EP₄ and IP₁ receptors in pig and rabbit blood vessels Br. J. Pharmacol. 134(2),313-324(2001).