RS-61756-007: a potent and selective thromboxane receptor (TP) agonist

The activity of RS-61756-007 (methyl-9-oxo, 15 alpha-hydroxy, 16-phenoxy, 17,18,19,20-tetranor prosta 4,5, 13(E) trienoate, 4,5,6(R), 8(R)) has been assessed at prostanoid receptors (DP, EP1, EP2, FP, IP and TP) in-vitro. The activity profile of RS-61756-007 resembles that of U46619, in that agonism was observed at TP and to a lesser extent at FP receptors, but there was no activity at the remaining subtypes. The actions of both RS-61756-007 and U46619 were antagonized in a similar manner by the TP antagonist SQ 29,548. We conclude that RS-61756-007 is a highly potent TP agonist.