Selfotel

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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
Moolimassa 223.16 g/mol [1][2]
Sulamispiste 290-292 °C

Selfotel (CGS-19755) on lääke, joka toimii kilpailevana NMDA-antagonistina ja kilpailee suoraan glutamaatin kanssa sitoutumisesta reseptoriin.[3] Alustavat tutkimukset osoittivat, että sillä oli kouristuksia estäviä, anksiolyyttisiä, kipua lievittäviä ja neuroprotektiivisia vaikutuksia,[4][5] ja sitä tutkittiin alun perin aivohalvauksen hoitoon,[6] mutta myöhemmät eläin- ja ihmistutkimukset osoittivat fensyklidiinin kaltaisia vaikutuksia,[7][8][9][10] sekä rajoitettua tehoa ja todisteita mahdollisesta neurotoksisuudesta joissakin olosuhteissa,[11][12][13] ja niin kliininen kehitys lopulta lopetettiin.[14][15]

Lähteet

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  1. ↑ https://commonchemistry.cas.org/detail?cas_rn=110347-85-8
  2. ↑ https://pubchem.ncbi.nlm.nih.gov/compound/68736
  3. ↑ Lehmann J., Hutchison A. J., McPherson S. E., Mondadori C., Schmutz M., Sinton C. M., 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.
  4. ↑ Bennett D. A., Lehmann J., Bernard P. S., Liebman J. M., Williams M., Wood P. L., 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.
  5. ↑ France C. P., Winger G. D., Woods J. H. (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.
  6. ↑ Grotta J., Clark W., Coull B., Pettigrew L. C., Mackay B., Goldstein L. B., 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.
  7. ↑ Bennett D. A., Bernard P. S., Amrick C. L., Wilson D. E., Liebman J. M., Hutchison A. J. (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.
  8. ↑ Koek W., Woods J. H., Colpaert F. C. (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.
  9. ↑ Lu Y., France C. P., Woods J. H. (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.
  10. ↑ Baron S. P., Woods J. H. (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.
  11. ↑ Morris G. F., Bullock R., Marshall S. B., Marmarou A., Maas A., Marshall L. F. (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.
  12. ↑ Davis S. M., Lees K. R., Albers G. W., Diener H. C., 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.
  13. ↑ Dawson D. A., Wadsworth G., Palmer A. M. (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.
  14. ↑ 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.
  15. ↑ Farin A., Marshall L. F. (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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