Novel prostanoid thromboxane A2 agonists.
The chemistry and biology of novel TXA2(TP)-receptor agonists based on the prostanoid skeleton is described and structure-activity-relationships are discussed. One compound,(5Z,13E), (9R,15R)-9-fluoro-15-hydroxy-16-phenoxy-17,18,19,20-tetranor- 5,13-prostadienoic acid (33), was identified which is 10 times more potent than the standard TP-receptor against U 46619.
Joachim
K D
KD
Research Laboratories of Schering AG, Berlin, Germany.
Klar
U
U
Pletsch
A
A
Rehwinkel
H
H
Skuballa
W
W
D001792:Blood Platelets / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects; D011457:Prostaglandins D / Q000138:chemical synthesis / Q000494:pharmacology*; D017482:Receptors, Thromboxane / Q000378:metabolism; D013928:Thromboxane A2 / Q000819:agonists*
C098307:9-fluoro-15-hydroxy-16-phenoxy-17,18,19,20-tetranor-5,13-prostadienoic acid; D011457:Prostaglandins D; D017482:Receptors, Thromboxane; D013928:Thromboxane A2