What question did this study set out to answer?

This research aims to compare the binding affinities and functional activities of treprostinil and iloprost at human prostanoid receptors.

March 27, 2012Biochemical PharmacologyOpen Access

Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: Treprostinil is a potent DP1 and EP2 agonist

View Full Paper

Ask AI

Bookmark

This research aims to compare the binding affinities and functional activities of treprostinil and iloprost at human prostanoid receptors.
Compared binding profile of iloprost and treprostinil at various human prostanoid receptors in cell lines.
Evaluated cyclic AMP levels and calcium influx in response to receptor activation.
Measured affinities using Ki values and potencies using EC50 values for both agonists.
Iloprost showed high binding affinity for EP1 (Ki 1.1 nM) and IP receptors (Ki 3.9 nM).
Treprostinil demonstrated high affinity for DP1 (Ki 4.4 nM), EP2 (Ki 3.6 nM), and IP receptors (Ki 32 nM).
Treprostinil exhibited superior potency in elevating cyclic AMP levels compared to iloprost, thus enhancing its vasorelaxant profile.

No takes yet. Share an insight, caveat, or question.

Randomized trial compares binding and activity of treprostinil and iloprost in human cell lines, suggesting differences in pulmonary vasodilation.

Whittle et al. (2012) studied this question.

View Full Paper

Ask AI

Bookmark

Randomized trial compares binding and activity of treprostinil and iloprost in human cell lines, suggesting differences in pulmonary vasodilation.