SCH-79797 explained

SCH-79797 is a drug which acts as a potent and selective antagonist of the thrombin receptor proteinase activated receptor 1 (PAR1).[1] It has anticoagulant, anticonvulsant and antiinflammatory effects and has been researched as a treatment for heart attack and stroke, though never developed for medical use.[2] [3] [4] [5] It also shows antibiotic actions which are not shared with other PAR1 antagonists such as vorapaxar, so may be mediated through a different target than PAR1.[6] [7]

Notes and References

  1. Ahn HS, Foster C, Boykow G, Stamford A, Manna M, Graziano M . Inhibition of cellular action of thrombin by N3-cyclopropyl-7--7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist . Biochemical Pharmacology . 60 . 10 . 1425–34 . November 2000 . 11020444 . 10.1016/s0006-2952(00)00460-3 .
  2. Yang JN, Chen J, Xiao M . A protease-activated receptor 1 antagonist protects against global cerebral ischemia/reperfusion injury after asphyxial cardiac arrest in rabbits . Neural Regeneration Research . 12 . 2 . 242–249 . February 2017 . 28400806 . 10.4103/1673-5374.199011 . 5361508 . free .
  3. Semenikhina M, Bogovyk R, Fedoriuk M, Nikolaienko O, Al Kury LT, Savotchenko A, Krishtal O, Isaeva E . 6 . Inhibition of protease-activated receptor 1 ameliorates behavioral deficits and restores hippocampal synaptic plasticity in a rat model of status epilepticus . Neuroscience Letters . 692 . 64–68 . January 2019 . 30391321 . 10.1016/j.neulet.2018.10.058 . 53217829 .
  4. Pontecorvi P, Banki MA, Zampieri C, Zalfa C, Azmoon P, Kounnas MZ, Marchese C, Gonias SL, Mantuano E . 6 . Fibrinolysis protease receptors promote activation of astrocytes to express pro-inflammatory cytokines . Journal of Neuroinflammation . 16 . 1 . 257 . December 2019 . 31810478 . 10.1186/s12974-019-1657-3 . 6896679 . free .
  5. Yokono Y, Hanada K, Narita M, Tatara Y, Kawamura Y, Miura N, Kitayama K, Nakata M, Nozaka M, Kato T, Kudo N, Tsushima M, Toyama Y, Itoh K, Tomita H . 6 . Blockade of PAR-1 Signaling Attenuates Cardiac Hypertrophy and Fibrosis in Renin-Overexpressing Hypertensive Mice . Journal of the American Heart Association . e015616 . June 2020 . 9 . 12 . 32495720 . 10.1161/JAHA.119.015616 . 7429042 . free .
  6. Gupta N, Liu R, Shin S, Sinha R, Pogliano J, Pogliano K, Griffin JH, Nizet V, Corriden R . 6 . SCH79797 improves outcomes in experimental bacterial pneumonia by boosting neutrophil killing and direct antibiotic activity . The Journal of Antimicrobial Chemotherapy . 73 . 6 . 1586–1594 . June 2018 . 29514266 . 10.1093/jac/dky033 . 5961356 . free .
  7. Martin JK, Sheehan JP, Bratton BP, Moore GM, Mateus A, Li SH, Kim H, Rabinowitz JD, Typas A, Savitski MM, Wilson MZ, Gitai Z . 6 . A Dual-Mechanism Antibiotic Kills Gram-Negative Bacteria and Avoids Drug Resistance . Cell . May 2020 . 181 . 7 . 1518–1532.e14 . 32497502 . 10.1016/j.cell.2020.05.005 . 219300022 . 7780349 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "SCH-79797".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.