title: BM 144: an original thromboxane A2 receptor antagonist derived from torasemide.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, University of Liège, Belgium.
authors.forename: J M
authors.initials: JM
authors.lastname: Dogné
authors.forename: P
authors.initials: P
authors.lastname: Neven
authors.forename: J
authors.initials: J
authors.lastname: Damas
authors.forename: J
authors.initials: J
authors.lastname: Fontaine
authors.forename: S
authors.initials: S
authors.lastname: Rolin
authors.forename: X
authors.initials: X
authors.lastname: De Leval
authors.forename: J
authors.initials: J
authors.lastname: Delarge
authors.forename: B
authors.initials: B
authors.lastname: Masereel
mesh_terms: 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
chemical_list: C120544:BM 144; D017482:Receptors, Thromboxane; D013449:Sulfonamides; D000077786:Torsemide