Literature DB >> 6143969

BM 13.177, a selective blocker of platelet and vessel wall thromboxane receptors, is active in man.

P Gresele, H Deckmyn, J Arnout, J Lemmens, W Janssens, J Vermylen.   

Abstract

BM 13.177, a sulphonamide derivative, prevented platelet aggregation by thromboxane A2 in vitro and selectively inhibited contraction of isolated rabbit femoral arteries induced by two stable endoperoxide analogues. In a double-blind placebo-controlled study, oral BM 13.177 inhibited platelet aggregation induced by arachidonic acid, low dose collagen, and the two stable endoperoxide analogues, and slightly prolonged the bleeding time. Generation of thromboxane or of other prostaglandins was not affected. No side-effects were seen. BM 13.177 appears selectively and safely to block platelet and vessel wall thromboxane receptors and should be useful in elucidating the role of thromboxane A2 in disease.

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Year:  1984        PMID: 6143969     DOI: 10.1016/s0140-6736(84)92328-6

Source DB:  PubMed          Journal:  Lancet        ISSN: 0140-6736            Impact factor:   79.321


  10 in total

Review 1.  Thromboxane synthase inhibitors and receptor antagonists.

Authors:  J Vermylen; H Deckmyn
Journal:  Cardiovasc Drugs Ther       Date:  1992-02       Impact factor: 3.727

Review 2.  Current concepts for a drug-induced inhibition of formation and action of thromboxane A2.

Authors:  H Patscheke
Journal:  Blut       Date:  1990-05

3.  Role of proaggregatory and antiaggregatory prostaglandins in hemostasis. Studies with combined thromboxane synthase inhibition and thromboxane receptor antagonism.

Authors:  P Gresele; J Arnout; H Deckmyn; E Huybrechts; G Pieters; J Vermylen
Journal:  J Clin Invest       Date:  1987-11       Impact factor: 14.808

4.  Changes in the venous compliance by bradykinin and angiotensin II and its significance for the vascular effects of cyclosporine-A.

Authors:  E Müller-Schweinitzer
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1988-12       Impact factor: 3.000

Review 5.  The role of eicosanoids in paediatrics.

Authors:  H W Seyberth; P G Kühl
Journal:  Eur J Pediatr       Date:  1988-05       Impact factor: 3.183

Review 6.  Novel antithrombotic drugs in development.

Authors:  M Verstraete; P Zoldhelyi
Journal:  Drugs       Date:  1995-06       Impact factor: 9.546

Review 7.  Current issues in thrombosis prevention with antiplatelet drugs.

Authors:  G de Gaetano; C Cerletti; E Dejana; J Vermylen
Journal:  Drugs       Date:  1986-06       Impact factor: 9.546

8.  Pharmacological characterization of cinnamophilin, a novel dual inhibitor of thromboxane synthase and thromboxane A2 receptor.

Authors:  S M Yu; T S Wu; C M Teng
Journal:  Br J Pharmacol       Date:  1994-03       Impact factor: 8.739

9.  Pharmacokinetics of the thromboxane A2 receptor antagonist sulotroban (BM 13.177) in renal failure.

Authors:  C Piper; C Staiger; Y Jumeau-Ziemendorff; V Uebis; B Kaufmann; K Stein
Journal:  Br J Clin Pharmacol       Date:  1989-09       Impact factor: 4.335

10.  Single dose pharmacokinetics and effects on platelet function of the thromboxane receptor blocker BM 13.177.

Authors:  C Staiger; H Patscheke; G Neugebauer; B Kaufmann; K Strein; R Endele; K Stegmeier
Journal:  Eur J Clin Pharmacol       Date:  1986       Impact factor: 2.953

  10 in total

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