Perzinfotel Explained

Perzinfotel (EAA-090) is a drug which acts as a potent NMDA antagonist.[1] It has neuroprotective effects and has been investigated for the treatment of stroke,[2] but lacks analgesic effects.[3] Nevertheless, it shows a good safety profile compared to older drugs, although further development of this drug has been discontinued.[4]

Prodrugs were developed since the oral bioavailability of perzinfotel is only around 3-5%.[5]

Notes and References

  1. Kinney WA, Abou-Gharbia M, Garrison DT, Schmid J, Kowal DM, Bramlett DR, Miller TL, Tasse RP, Zaleska MM, Moyer JA . 6 . Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid (EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere . Journal of Medicinal Chemistry . 41 . 2 . 236–46 . January 1998 . 9457246 . 10.1021/jm970504g .
  2. Sun L, Chiu D, Kowal D, Simon R, Smeyne M, Zukin RS, Olney J, Baudy R, Lin S . Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride) . The Journal of Pharmacology and Experimental Therapeutics . 310 . 2 . 563–70 . August 2004 . 15075380 . 10.1124/jpet.104.066092 . 25505657 .
  3. Brandt MR, Cummons TA, Potestio L, Sukoff SJ, Rosenzweig-Lipson S . Effects of the N-methyl-D-aspartate receptor antagonist perzinfotel [EAA-090; [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid] on chemically induced thermal hypersensitivity . The Journal of Pharmacology and Experimental Therapeutics . 313 . 3 . 1379–86 . June 2005 . 15764736 . 10.1124/jpet.105.084467 . 12989500.
  4. Web site: Perzinfotel . Adis International Ltd. . Springer Nature Switzerland AG .
  5. Baudy RB, Butera JA, Abou-Gharbia MA, Chen H, Harrison B, Jain U, Magolda R, Sze JY, Brandt MR, Cummons TA, Kowal D, Pangalos MN, Zupan B, Hoffmann M, May M, Mugford C, Kennedy J, Childers WE . 6 . Prodrugs of perzinfotel with improved oral bioavailability . Journal of Medicinal Chemistry . 52 . 3 . 771–8 . February 2009 . 19146418 . 10.1021/jm8011799 .

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