Wikipedia

Selfotel

kemiallinen yhdiste

Selfotel (CGS-19755) on lääke, joka toimii kilpailevana NMDA-antagonistina ja kilpailee suoraan glutamaatin kanssa sitoutumisesta reseptoriin.[1] Alustavat tutkimukset osoittivat, että sillä oli kouristuksia estäviä, anksiolyyttisiä, kipua lievittäviä ja neuroprotektiivisia vaikutuksia,[2][3] ja sitä tutkittiin alun perin aivohalvauksen hoitoon,[4] mutta myöhemmät eläin- ja ihmistutkimukset osoittivat fensyklidiinin kaltaisia vaikutuksia,[5][6][7][8] sekä rajoitettua tehoa ja todisteita mahdollisesta neurotoksisuudesta joissakin olosuhteissa,[9][10][11] ja niin kliininen kehitys lopulta lopetettiin.[12][13]

Selfotel
Tunnisteet
IUPAC-nimi (2S,4R)-4-(fosfonometyyli)piperidiini-2-karboksyylihappo
Muut nimet CGS-19755
CAS-numero 110347-85-8
PubChem CID 68736
SMILES C(P(=O)(O)O)C1CC(C(O)=O)NCC1
Ominaisuudet
Molekyylikaava C7H14NO5P
Sulamispiste 290-292 °C

Lähteet muokkaa

  1. ↑ Lehmann J, Hutchison AJ, McPherson SE, Mondadori C, Schmutz M, Sinton CM, et al. (July 1988). "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. PMID 2899170.
  2. ↑ Bennett DA, Lehmann J, Bernard PS, Liebman JM, Williams M, Wood PL, et al. (1990). "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. PMID 1981269.
  3. ↑ France CP, Winger GD, Woods JH (September 1990). "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. doi:10.1016/0006-8993(90)91247-e. hdl:2027.42/28393. PMID 2257491.
  4. ↑ Grotta J, Clark W, Coull B, Pettigrew LC, Mackay B, Goldstein LB, et al. (April 1995). "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. doi:10.1161/01.str.26.4.602. PMID 7709405.
  5. ↑ Bennett DA, Bernard PS, Amrick CL, Wilson DE, Liebman JM, Hutchison AJ (August 1989). "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. PMID 2547931.
  6. ↑ Koek W, Woods JH, Colpaert FC (June 1990). "N-methyl-D-aspartate antagonism and phencyclidine-like activity: a drug discrimination analysis". The Journal of Pharmacology and Experimental Therapeutics. 253 (3): 1017–25. PMID 2193142.
  7. ↑ Lu Y, France CP, Woods JH (November 1992). "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. PMID 1432686.
  8. ↑ Baron SP, Woods JH (March 1995). "Competitive and uncompetitive N-methyl-D-aspartate antagonist discriminations in pigeons: CGS 19755 and phencyclidine". Psychopharmacology. 118 (1): 42–51. doi:10.1007/bf02245248. hdl:2027.42/46346. PMID 7597121.
  9. ↑ Morris GF, Bullock R, Marshall SB, Marmarou A, Maas A, Marshall LF (November 1999). "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. doi:10.3171/jns.1999.91.5.0737. PMID 10541229.
  10. ↑ Davis SM, Lees KR, Albers GW, Diener HC, Markabi S, Karlsson G, Norris J (February 2000). "Selfotel in acute ischemic stroke : possible neurotoxic effects of an NMDA antagonist". Stroke. 31 (2): 347–54. doi:10.1161/01.str.31.2.347. PMID 10657404.
  11. ↑ Dawson DA, Wadsworth G, Palmer AM (February 2001). "A comparative assessment of the efficacy and side-effect liability of neuroprotective compounds in experimental stroke". Brain Research. 892 (2): 344–50. doi:10.1016/s0006-8993(00)03269-8. PMID 11172782.
  12. ↑ Ikonomidou C, Turski L (October 2002). "Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury?". The Lancet. Neurology. 1 (6): 383–6. doi:10.1016/s1474-4422(02)00164-3. PMID 12849400.
  13. ↑ Farin A, Marshall LF (2004). "Lessons from epidemiologic studies in clinical trials of traumatic brain injury". Acta Neurochirurgica. Supplement. 89: 101–7. doi:10.1007/978-3-7091-0603-7_14. ISBN 978-3-7091-7206-3. PMID 15335108.
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