Location via proxy:   [ UP ]  
[Report a bug]   [Manage cookies]                
Pređi na sadržaj

GTS-21

S Vikipedije, slobodne enciklopedije
GTS-21
IUPAC ime
3-[(3E)-3-[(2,4-dimetoksifenil)metiliden]-5,6-dihidro-4H-piridin-2-il]piridin
Identifikatori
ATC kodNone
PubChemCID 5310985
Sinonimi3-(2,4-dimetoksi-benziliden)anabasein
Hemijski podaci
FormulaC19H20N2O2
Molarna masa308,374
  • COc2cc(OC)ccc2C=C1CCCN=C1c3cnccc3

GTS-21 (DMXB-A) je lek koji deluje kao parcijalni agonist na neuronskim nikotinskim acetilholinskim receptorima. On se vezuje za α4β2 i α7 receptore, ali znatno aktivira samo α7.[1][2]

GTS-21 i njegov demetilisani aktivni metabolit 4-OH-GTS-21[3] manifestuju nootropne[4] i neuroprotektivne efekte,[5][6][7][8] i GTS-21 se ispituje za moguću primenu u tretmanu Alchajmerove bolesti,[9] nikotinske zavisnosti,[10] kao i šizofrenije.[11][12][13][14][15]

Reference

[uredi | uredi izvor]
  1. ^ Briggs CA, Anderson DJ, Brioni JD, Buccafusco JJ, Buckley MJ, Campbell JE, Decker MW, Donnelly-Roberts D, Elliott RL, Gopalakrishnan M, Holladay MW, Hui YH, Jackson WJ, Kim DJ, Marsh KC, O'Neill A, Prendergast MA, Ryther KB, Sullivan JP, Arneric SP. Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacology, Biochemistry and Behaviour. 1997 May-Jun;57(1-2):231-41. . PMID 9164577.  Nedostaje ili je prazan parametar |title= (pomoć)
  2. ^ Meyer, E. M.; Tay ET; Papke, R. L.; Meyers, C; Huang GL, de Fiebre CM (септембар 1997). „3-[2,4-Dimethoxybenzylidene]anabaseine (DMXB) selectively activates rat alpha7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner”. Brain Research. 768 (1-2): 49—56. PMID 9369300. .
  3. ^ Meyer EM, Kuryatov A, Gerzanich V, Lindstrom J, Papke RL. Analysis of 3-(4-hydroxy, 2-Methoxybenzylidene)anabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors. Journal of Pharmacology and Experimental Therapeutics. decembar 1998.  Nedostaje ili je prazan parametar |title= (pomoć) . 287 (3): 918—25. PMID 9864273.  Nedostaje ili je prazan parametar |title= (pomoć)
  4. ^ Kitagawa H, Takenouchi T, Azuma R, Wesnes KA, Kramer WG, Clody DE, Burnett AL. Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. Neuropsychopharmacology. 2003 Mar. . 28 (3): 542—51. PMID 12629535.  Nedostaje ili je prazan parametar |title= (pomoć)
  5. ^ Meyer, E. M.; King, M. A.; Meyers, C. (март 1998). „Neuroprotective effects of 2,4-dimethoxybenzylidene anabaseine (DMXB) and tetrahydroaminoacridine (THA) in neocortices of nucleus basalis lesioned rats”. Brain Research. 786 (1-2): 252—4. PMID 9555043. .
  6. ^ Shimohama S, Greenwald DL, Shafron DH, Akaika A, Maeda T, Kaneko S, Kimura J, Simpkins CE, Day AL, Meyer EM (јануар 1998). „Nicotinic alpha 7 receptors protect against glutamate neurotoxicity and neuronal ischemic damage”. Brain Research. 779 (1-2): 359—63. PMID 9473725. .
  7. ^ Li Y, Meyer EM, Walker DW, Millard WJ, He YJ, King MA (maj 2002). „Alpha7 nicotinic receptor activation inhibits ethanol-induced mitochondrial dysfunction, cytochrome c release and neurotoxicity in primary rat hippocampal neuronal cultures”. Journal of Neurochemistry.  . 81 (4): 853—8. PMID 12065644.  Nedostaje ili je prazan parametar |title= (pomoć)
  8. ^ de Fiebre NC, de Fiebre CM. Alpha 7 nicotinic acetylcholine receptor-mediated protection against ethanol-induced neurotoxicity. Alcohol. 2003 Nov. . 31 (3): 149—53. PMID 14693263.  Nedostaje ili je prazan parametar |title= (pomoć)
  9. ^ Kem WR. The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behavioural Brain Research. 113 (1-2): 169—81. август 2000. PMID 10942043.  Недостаје или је празан параметар |title= (помоћ).
  10. ^ Foulds J, Burke M, Steinberg M, Williams JM, Ziedonis DM. Advances in pharmacotherapy for tobacco dependence. Expert Opinion on Emerging Drugs. 2004 May. . 9 (1): 39—53. PMID 15155135.  Nedostaje ili je prazan parametar |title= (pomoć)
  11. ^ Simosky JK, Stevens KE, Freedman R. Nicotinic agonists and psychosis. Current Drug Targets. CNS and Neurological Disorders. 2002 Apr. . 1 (2): 149—62. PMID 12769624.  Nedostaje ili je prazan parametar |title= (pomoć)
  12. ^ Martin LF, Kem WR, Freedman R. Alpha-7 nicotinic receptor agonists: potential new candidates for the treatment of schizophrenia. Psychopharmacology (Berlin). 2004 Jun. . 174 (1): 54—64. PMID 15205879.  Nedostaje ili je prazan parametar |title= (pomoć)
  13. ^ Olincy A, Harris JG, Johnson LL, Pender V, Kongs S, Allensworth D, Ellis J, Zerbe GO, Leonard S, Stevens KE, Stevens JO, Martin L, Adler LE, Soti F, Kem WR, Freedman R. Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia. Archives of General Psychiatry. 2006 Jun. . 63 (6): 630—8. PMID 16754836.  Nedostaje ili je prazan parametar |title= (pomoć)
  14. ^ Olincy, A.; Stevens, K. E. (15. 10. 2007). „Treating schizophrenia symptoms with an alpha7 nicotinic agonist, from mice to men”. Biochemical Pharmacology. 74 (8): 1192—201. PMID 17714692. 
  15. ^ Freedman R, Olincy A, Buchanan RW, Harris JG, Gold JM, Johnson L, Allensworth D, Guzman-Bonilla A, Clement B, Ball MP, Kutnick J, Pender V, Martin LF, Stevens KE, Wagner BD, Zerbe GO, Soti F, Kem WR. Initial Phase 2 Trial of a Nicotinic Agonist in Schizophrenia. American Journal of Psychiatry. 2008 Apr 1. [Epub ahead of print] . PMID 18381905.  Nedostaje ili je prazan parametar |title= (pomoć)

Spoljašnje veze

[uredi | uredi izvor]
Preuzeto iz „https://sr.wikipedia.org/w/index.php?title=GTS-21&oldid=28302444”