Selfotel (CGS-19755) on lääke, joka toimii kilpailevana NMDA-antagonistina ja kilpailee suoraan glutamaatin kanssa sitoutumisesta reseptoriin.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. Alustavat tutkimukset osoittivat, että sillä oli kouristuksia estäviä, anksiolyyttisiä, kipua lievittäviä ja neuroprotektiivisia vaikutuksia,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. 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. ja sitä tutkittiin alun perin aivohalvauksen hoitoon,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. mutta myöhemmät eläin- ja ihmistutkimukset osoittivat fensyklidiinin kaltaisia vaikutuksia,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. 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. 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. 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. sekä rajoitettua tehoa ja todisteita mahdollisesta neurotoksisuudesta joissakin olosuhteissa,Morris G. F. et al. (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. Davis S. M. et al. (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. 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. ja niin kliininen kehitys lopulta lopetettiin.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. 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. .
Katso myös Midafotel
Lähteet
Luokka:Dissosiatiivit Luokka:Hylätyt lääkkeet Luokka:NMDA-reseptorin antagonistit