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Selfotel
Clinical data
Other namesSelfotel
Legal status
Legal status
  • In general: legal
Identifiers
  • (2S,4R)-4-(phosphonomethyl)piperidine-2-carboxylic acid
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard ( EPA)
Chemical and physical data
FormulaC7H14NO5P
Molar mass223.165 g·mol−1
3D model ( JSmol)
  • C1CN[C@@H](C[C@@H]1CP(=O)(O)O)C(=O)O
  • InChI=1S/C7H14NO5P/c9-7(10)6-3-5(1-2-8-6)4-14(11,12)13/h5-6,8H,1-4H2,(H,9,10)(H2,11,12,13)/t5-,6+/m1/s1 ☒N
  • Key:LPMRCCNDNGONCD-RITPCOANSA-N ☒N
 ☒NcheckY  (what is this?)   (verify)

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]

References

  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. S2CID  8793348.
  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. S2CID  31477519.
  13. ^ Farin A, Marshall LF (2004). "Lessons from epidemiologic studies in clinical trials of traumatic brain injury". Mechanisms of Secondary Brain Damage from Trauma and Ischemia. Vol. 89. pp. 101–7. doi: 10.1007/978-3-7091-0603-7_14. ISBN  978-3-7091-7206-3. PMID  15335108. {{ cite book}}: |journal= ignored ( help)


Stub icon

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

Retrieved from " https://en.wikipedia.org/?title=Selfotel&oldid=1207002651"
From Wikipedia, the free encyclopedia
Selfotel
Clinical data
Other namesSelfotel
Legal status
Legal status
  • In general: legal
Identifiers
  • (2S,4R)-4-(phosphonomethyl)piperidine-2-carboxylic acid
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard ( EPA)
Chemical and physical data
FormulaC7H14NO5P
Molar mass223.165 g·mol−1
3D model ( JSmol)
  • C1CN[C@@H](C[C@@H]1CP(=O)(O)O)C(=O)O
  • InChI=1S/C7H14NO5P/c9-7(10)6-3-5(1-2-8-6)4-14(11,12)13/h5-6,8H,1-4H2,(H,9,10)(H2,11,12,13)/t5-,6+/m1/s1 ☒N
  • Key:LPMRCCNDNGONCD-RITPCOANSA-N ☒N
 ☒NcheckY  (what is this?)   (verify)

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]

References

  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. S2CID  8793348.
  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. S2CID  31477519.
  13. ^ Farin A, Marshall LF (2004). "Lessons from epidemiologic studies in clinical trials of traumatic brain injury". Mechanisms of Secondary Brain Damage from Trauma and Ischemia. Vol. 89. pp. 101–7. doi: 10.1007/978-3-7091-0603-7_14. ISBN  978-3-7091-7206-3. PMID  15335108. {{ cite book}}: |journal= ignored ( help)


Stub icon

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

Retrieved from " https://en.wikipedia.org/?title=Selfotel&oldid=1207002651"

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