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Selfotel — разлика између измена

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'''Selfotel''' je [[organsko jedinjenje]], koje sadrži 7 [[atom]]a [[ugljenik]]a i ima [[Молекулска маса|molekulsku masu]] od 223,164 [[Јединица атомске масе|-{''Da''}-]].
'''Selfotel''' ('''CGS-19755''') je lek koji deluje kao kompetitivni [[NMDA antagonist]], koji se direktno nadmeće sa [[glutamate|glutamatom]] za vezivanje za receptor.<ref>{{cite journal | vauthors = Lehmann J, Hutchison AJ, McPherson SE, Mondadori C, Schmutz M, Sinton CM, Tsai C, Murphy DE, Steel DJ, Williams M | display-authors = 6 | title = CGS 19755, a selective and competitive N-methyl-D-aspartate-type excitatory amino acid receptor antagonist | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 246 | issue = 1 | pages = 65–75 | date = July 1988 | pmid = 2899170 }}</ref> Inicijalne studije su pokazale da ima [[anticonvulsant|antikonvulzivne]], [[anxiolytic|anksiolitičke]], [[analgesic|analgetičke]] i [[neuroprotective|neuroprotektivne]] efekte,<ref>{{cite journal | vauthors = Bennett DA, Lehmann J, Bernard PS, Liebman JM, Williams M, Wood PL, Boast CA, Hutchison AJ | display-authors = 6 | title = CGS 19755: a novel competitive N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant, anxiolytic and anti-ischemic properties | journal = Progress in Clinical and Biological Research | volume = 361 | pages = 519–24 | pmid = 1981269 | year = 1990 }}</ref><ref>{{cite journal | vauthors = France CP, Winger GD, Woods JH | title = Analgesic, anesthetic, and respiratory effects of the competitive N-methyl-D-aspartate (NMDA) antagonist CGS 19755 in rhesus monkeys | journal = Brain Research | volume = 526 | issue = 2 | pages = 355–8 | date = September 1990 | pmid = 2257491 | doi = 10.1016/0006-8993(90)91247-e | hdl = 2027.42/28393 | hdl-access = free }}</ref> i prvobitno je istraživan za lečenje [[stroke|moždanog udara]],<ref>{{cite journal | vauthors = Grotta J, Clark W, Coull B, Pettigrew LC, Mackay B, Goldstein LB, Meissner I, Murphy D, LaRue L | display-authors = 6 | title = Safety and tolerability of the glutamate antagonist CGS 19755 (Selfotel) in patients with acute ischemic stroke. Results of a phase IIa randomized trial | journal = Stroke | volume = 26 | issue = 4 | pages = 602–5 | date = April 1995 | pmid = 7709405 | doi = 10.1161/01.str.26.4.602 }}</ref> ali kasnije studije na životinjama i ljudima pokazale su efekte slične [[phencyclidine|fenciklidinu]],<ref>{{cite journal | vauthors = Bennett DA, Bernard PS, Amrick CL, Wilson DE, Liebman JM, Hutchison AJ | title = Behavioral pharmacological profile of CGS 19755, a competitive antagonist at N-methyl-D-aspartate receptors | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 250 | issue = 2 | pages = 454–60 | date = August 1989 | pmid = 2547931 }}</ref><ref>{{cite journal | vauthors = Koek W, Woods JH, Colpaert FC | title = N-methyl-D-aspartate antagonism and phencyclidine-like activity: a drug discrimination analysis | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 253 | issue = 3 | pages = 1017–25 | date = June 1990 | pmid = 2193142 }}</ref><ref>{{cite journal | vauthors = Lu Y, France CP, Woods JH | title = 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 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 263 | issue = 2 | pages = 499–504 | date = November 1992 | pmid = 1432686 }}</ref><ref>{{cite journal | vauthors = Baron SP, Woods JH | title = Competitive and uncompetitive N-methyl-D-aspartate antagonist discriminations in pigeons: CGS 19755 and phencyclidine | journal = Psychopharmacology | volume = 118 | issue = 1 | pages = 42–51 | date = March 1995 | pmid = 7597121 | doi = 10.1007/bf02245248 | hdl = 2027.42/46346 | hdl-access = free }}</ref> kao i ograničenu efikasnost i evidenciju o mogućoj [[neurotoxicity|neurotoksičnosti]] pod nekim uslovima,<ref>{{cite journal | vauthors = Morris GF, Bullock R, Marshall SB, Marmarou A, Maas A, Marshall LF | title = 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 = Journal of Neurosurgery | volume = 91 | issue = 5 | pages = 737–43 | date = November 1999 | pmid = 10541229 | doi = 10.3171/jns.1999.91.5.0737 }}</ref><ref>{{cite journal | vauthors = Davis SM, Lees KR, Albers GW, Diener HC, Markabi S, Karlsson G, Norris J | title = Selfotel in acute ischemic stroke : possible neurotoxic effects of an NMDA antagonist | journal = Stroke | volume = 31 | issue = 2 | pages = 347–54 | date = February 2000 | pmid = 10657404 | doi = 10.1161/01.str.31.2.347 | doi-access = free }}</ref><ref>{{cite journal | vauthors = Dawson DA, Wadsworth G, Palmer AM | title = A comparative assessment of the efficacy and side-effect liability of neuroprotective compounds in experimental stroke | journal = Brain Research | volume = 892 | issue = 2 | pages = 344–50 | date = February 2001 | pmid = 11172782 | doi = 10.1016/s0006-8993(00)03269-8 }}</ref> te je klinički razvoj na kraju prekinut.<ref>{{cite journal | vauthors = Ikonomidou C, Turski L | title = Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? | journal = The Lancet. Neurology | volume = 1 | issue = 6 | pages = 383–6 | date = October 2002 | pmid = 12849400 | doi = 10.1016/s1474-4422(02)00164-3 }}</ref><ref>{{cite journal | vauthors = Farin A, Marshall LF | title = Lessons from epidemiologic studies in clinical trials of traumatic brain injury | journal = Acta Neurochirurgica. Supplement | volume = 89 | pages = 101–7 | pmid = 15335108 | doi = 10.1007/978-3-7091-0603-7_14 | year = 2004 | isbn = 978-3-7091-7206-3 }}</ref>

== Osobine ==
== Osobine ==

⚫
Selfotel je [[organsko jedinjenje]], koje sadrži 7 [[atom]]a [[ugljenik]]a i ima [[Молекулска маса|molekulsku masu]] od 223,164 [[Јединица атомске масе|-{''Da''}-]].


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Верзија на датум 17. децембар 2023. у 06:59

Selfotel
Klinički podaci
Drugs.comMonografija
Identifikatori
CAS broj110347-85-8 ДаY
ATC kodNone
PubChemCID 68736
UNII4VGJ4A41L2 ДаY
KEGGD02410 ДаY
ChEMBLCHEMBL39664 ДаY
SinonimiSelfotel
Hemijski podaci
FormulaC7H14NO5P
Molarna masa223,164
  • OC(=O)[C@@H]1C[C@H](CP(=O)(O)O)CCN1
  • 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 ДаY
  • Key:LPMRCCNDNGONCD-RITPCOANSA-N ДаY

Selfotel (CGS-19755) je lek koji deluje kao kompetitivni NMDA antagonist, koji se direktno nadmeće sa glutamatom za vezivanje za receptor.[1] Inicijalne studije su pokazale da ima antikonvulzivne, anksiolitičke, analgetičke i neuroprotektivne efekte,[2][3] i prvobitno je istraživan za lečenje moždanog udara,[4] ali kasnije studije na životinjama i ljudima pokazale su efekte slične fenciklidinu,[5][6][7][8] kao i ograničenu efikasnost i evidenciju o mogućoj neurotoksičnosti pod nekim uslovima,[9][10][11] te je klinički razvoj na kraju prekinut.[12][13]

Osobine

Selfotel je organsko jedinjenje, koje sadrži 7 atoma ugljenika i ima molekulsku masu od 223,164 Da.

Osobina Vrednost
Broj akceptora vodonika 6
Broj donora vodonika 4
Broj rotacionih veza 3
Particioni koeficijent[14] (ALogP) -3,5
Rastvorljivost[15] (logS, log(mol/L)) 0,2
Polarna površina[16] (PSA, Å2) 116,7

Reference

  1. ^ Lehmann J, Hutchison AJ, McPherson SE, Mondadori C, Schmutz M, Sinton CM, et al. (јул 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 (септембар 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. PMID 2257491. doi:10.1016/0006-8993(90)91247-e. hdl:2027.42/28393 Слободан приступ. 
  4. ^ Grotta J, Clark W, Coull B, Pettigrew LC, Mackay B, Goldstein LB, et al. (април 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. PMID 7709405. doi:10.1161/01.str.26.4.602. 
  5. ^ Bennett DA, Bernard PS, Amrick CL, Wilson DE, Liebman JM, Hutchison AJ (август 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 (јун 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 (новембар 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 (март 1995). „Competitive and uncompetitive N-methyl-D-aspartate antagonist discriminations in pigeons: CGS 19755 and phencyclidine”. Psychopharmacology. 118 (1): 42—51. PMID 7597121. doi:10.1007/bf02245248. hdl:2027.42/46346 Слободан приступ. 
  9. ^ Morris GF, Bullock R, Marshall SB, Marmarou A, Maas A, Marshall LF (новембар 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. PMID 10541229. doi:10.3171/jns.1999.91.5.0737. 
  10. ^ Davis SM, Lees KR, Albers GW, Diener HC, Markabi S, Karlsson G, Norris J (фебруар 2000). „Selfotel in acute ischemic stroke : possible neurotoxic effects of an NMDA antagonist”. Stroke. 31 (2): 347—54. PMID 10657404. doi:10.1161/01.str.31.2.347 Слободан приступ. 
  11. ^ Dawson DA, Wadsworth G, Palmer AM (фебруар 2001). „A comparative assessment of the efficacy and side-effect liability of neuroprotective compounds in experimental stroke”. Brain Research. 892 (2): 344—50. PMID 11172782. doi:10.1016/s0006-8993(00)03269-8. 
  12. ^ Ikonomidou C, Turski L (октобар 2002). „Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury?”. The Lancet. Neurology. 1 (6): 383—6. PMID 12849400. doi:10.1016/s1474-4422(02)00164-3. 
  13. ^ Farin A, Marshall LF (2004). „Lessons from epidemiologic studies in clinical trials of traumatic brain injury”. Acta Neurochirurgica. Supplement. 89: 101—7. ISBN 978-3-7091-7206-3. PMID 15335108. doi:10.1007/978-3-7091-0603-7_14. 
  14. ^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o. 
  15. ^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t. 
  16. ^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e. 

Literatura

Spoljašnje veze

Selfotel на Викимедијиној остави.
Преузето из „https://sr.wikipedia.org/w/index.php?title=Selfotel&oldid=26597264”