BM 144: an original thromboxane A2 receptor antagonist derived from torasemide.
Torasemide, a new sulfonylurea high ceiling loop diuretic, has been demonstrated to induce a concentration dependent relaxation of canine coronary precontracted with thromboxane A2 (TXA2). With the aim to develop more potent TXA2 receptor antagonists, we investigated a series of torasemide derivatives. This pharmacomodulation led to the discovery of a sulfonyl-cyanoguanidine (BM 144) which presents the same pharmacological profile as sulotroban, a TXA2 receptor antagonist used as reference.
Dogné
J M
JM
Department of Medicinal Chemistry, University of Liège, Belgium.
Neven
P
P
Damas
J
J
Fontaine
J
J
Rolin
S
S
De Leval
X
X
Delarge
J
J
Masereel
B
B
D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects; D017482:Receptors, Thromboxane / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000077786:Torsemide
C120544:BM 144; D017482:Receptors, Thromboxane; D013449:Sulfonamides; D000077786:Torsemide