BM 144：一种源自托拉塞米的新型血栓素A2受体拮抗剂。
BM 144: an original thromboxane A2 receptor antagonist derived from torasemide.
作者信息
Dogné J M, Neven P, Damas J, Fontaine J, Rolin S, De Leval X, Delarge J, Masereel B
机构信息
Department of Medicinal Chemistry, University of Liège, Belgium.
出版信息
J Pharm Belg. 1999 Mar-Apr;54(2):57-8.
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.
托拉塞米是一种新型的磺酰脲类高效能髓袢利尿剂，已证明它能使预先用血栓素A2（TXA2）收缩的犬冠状动脉产生浓度依赖性舒张。为了开发更有效的TXA2受体拮抗剂，我们研究了一系列托拉塞米衍生物。这种药效调制导致发现了一种磺酰基氰基胍（BM 144），它具有与作为参考的TXA2受体拮抗剂舒洛地尔相同的药理学特征。
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