Selfotel Explained

Selfotel (CGS-19755) is a drug which acts as a competitive NMDA antagonist, directly competing with glutamate for binding to the receptor.[1] Initial studies showed it to have anticonvulsant, anxiolytic, analgesic and neuroprotective effects,[2] [3] and it was originally researched for the treatment of stroke,[4] but subsequent animal and human studies showed phencyclidine-like effects,[5] [6] [7] [8] as well as limited efficacy and evidence for possible neurotoxicity under some conditions,[9] [10] [11] and so clinical development was ultimately discontinued.[12] [13]

Notes and References

  1. Lehmann J, Hutchison AJ, McPherson SE, Mondadori C, Schmutz M, Sinton CM, Tsai C, Murphy DE, Steel DJ, Williams M . 6 . CGS 19755, a selective and competitive N-methyl-D-aspartate-type excitatory amino acid receptor antagonist . The Journal of Pharmacology and Experimental Therapeutics . 246 . 1 . 65–75 . July 1988 . 2899170 .
  2. Bennett DA, Lehmann J, Bernard PS, Liebman JM, Williams M, Wood PL, Boast CA, Hutchison AJ . 6 . CGS 19755: a novel competitive N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant, anxiolytic and anti-ischemic properties . Progress in Clinical and Biological Research . 361 . 519–24 . 1981269 . 1990 .
  3. France CP, Winger GD, Woods JH . Analgesic, anesthetic, and respiratory effects of the competitive N-methyl-D-aspartate (NMDA) antagonist CGS 19755 in rhesus monkeys . Brain Research . 526 . 2 . 355–8 . September 1990 . 2257491 . 10.1016/0006-8993(90)91247-e . 2027.42/28393 . free .
  4. Grotta J, Clark W, Coull B, Pettigrew LC, Mackay B, Goldstein LB, Meissner I, Murphy D, LaRue L . 6 . Safety and tolerability of the glutamate antagonist CGS 19755 (Selfotel) in patients with acute ischemic stroke. Results of a phase IIa randomized trial . Stroke . 26 . 4 . 602–5 . April 1995 . 7709405 . 10.1161/01.str.26.4.602 .
  5. Bennett DA, Bernard PS, Amrick CL, Wilson DE, Liebman JM, Hutchison AJ . Behavioral pharmacological profile of CGS 19755, a competitive antagonist at N-methyl-D-aspartate receptors . The Journal of Pharmacology and Experimental Therapeutics . 250 . 2 . 454–60 . August 1989 . 2547931 .
  6. Koek W, Woods JH, Colpaert FC . N-methyl-D-aspartate antagonism and phencyclidine-like activity: a drug discrimination analysis . The Journal of Pharmacology and Experimental Therapeutics . 253 . 3 . 1017–25 . June 1990 . 2193142 .
  7. Lu Y, France CP, Woods JH . Tolerance to the cataleptic effect of the N-methyl-D-aspartate (NMDA) receptor antagonists in pigeons: cross-tolerance between PCP-like compounds and competitive NMDA antagonists . The Journal of Pharmacology and Experimental Therapeutics . 263 . 2 . 499–504 . November 1992 . 1432686 .
  8. Baron SP, Woods JH . Competitive and uncompetitive N-methyl-D-aspartate antagonist discriminations in pigeons: CGS 19755 and phencyclidine . Psychopharmacology . 118 . 1 . 42–51 . March 1995 . 7597121 . 10.1007/bf02245248 . 2027.42/46346 . free .
  9. Morris GF, Bullock R, Marshall SB, Marmarou A, Maas A, Marshall LF . Failure of the competitive N-methyl-D-aspartate antagonist Selfotel (CGS 19755) in the treatment of severe head injury: results of two phase III clinical trials. The Selfotel Investigators . Journal of Neurosurgery . 91 . 5 . 737–43 . November 1999 . 10541229 . 10.3171/jns.1999.91.5.0737 .
  10. Davis SM, Lees KR, Albers GW, Diener HC, Markabi S, Karlsson G, Norris J . Selfotel in acute ischemic stroke : possible neurotoxic effects of an NMDA antagonist . Stroke . 31 . 2 . 347–54 . February 2000 . 10657404 . 10.1161/01.str.31.2.347 . free .
  11. Dawson DA, Wadsworth G, Palmer AM . A comparative assessment of the efficacy and side-effect liability of neuroprotective compounds in experimental stroke . Brain Research . 892 . 2 . 344–50 . February 2001 . 11172782 . 10.1016/s0006-8993(00)03269-8 . 8793348 .
  12. Ikonomidou C, Turski L . Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? . The Lancet. Neurology . 1 . 6 . 383–6 . October 2002 . 12849400 . 10.1016/s1474-4422(02)00164-3 . 31477519 .
  13. Book: Farin A, Marshall LF . Lessons from epidemiologic studies in clinical trials of traumatic brain injury . Mechanisms of Secondary Brain Damage from Trauma and Ischemia . Acta Neurochirurgica. Supplement . 89 . 101–7 . 15335108 . 10.1007/978-3-7091-0603-7_14 . 2004 . 978-3-7091-7206-3 .

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