S-18986

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S-18986
(IUPAC) ime
(S)-2,3-dihidro-[3,4]ciklopentano-1,2,4-benzotiadiazin-1,1-dioksid
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 637863
Hemijski podaci
Formula C10H12N2O2S 
Mol. masa 224,279 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Novi lek u ispitivanju

S-18986 je ampakinski lek koji je srodan sa ciklotiazidom. On ima nootropne i neuroprotektivne efekte u životinjskim studijama. S-18986 indukuje pojavu BDNF i AMPA posredovanog otpuštanja noradrenalina i acetilholina u hipokampusu i frontalnom korteksu mozga.[3][4][5][6][7][8][9][10][11][12]

Reference[uredi - уреди | uredi izvor]

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Lockhart B, Iop F, Closier M, Lestage P (August 2000). "(S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide: (S18986-1) a positive modulator of AMPA receptors enhances (S)-AMPA-mediated [3H]noradrenaline release from rat hippocampal and frontal cortex slices". European Journal of Pharmacology 401 (2): 145–53. DOI:10.1016/S0014-2999(00)00433-7. PMID 10924919. 
  4. ↑ Lebrun C, Pillière E, Lestage P (August 2000). "Effects of S 18986-1, a novel cognitive enhancer, on memory performances in an object recognition task in rats". European Journal of Pharmacology 401 (2): 205–12. DOI:10.1016/S0014-2999(00)00429-5. PMID 10924928. 
  5. ↑ Dicou E, Rangon CM, Guimiot F, Spedding M, Gressens P (April 2003). "Positive allosteric modulators of AMPA receptors are neuroprotective against lesions induced by an NMDA agonist in neonatal mouse brain". Brain Research 970 (1-2): 221–5. DOI:10.1016/S0006-8993(03)02357-6. PMID 12706264. 
  6. ↑ Rosi S, Giovannini MG, Lestage PJ, Muñoz C, Corte LD, Pepeu G (May 2004). "S 18986, a positive modulator of AMPA receptors with cognition-enhancing properties, increases ACh release in the hippocampus of young and aged rat". Neuroscience Letters 361 (1-3): 120–3. DOI:10.1016/j.neulet.2003.12.061. PMID 15135908. 
  7. ↑ Bourasset F, Bernard K, Muñoz C, Genissel P, Scherrmann JM (August 2005). "Neuropharmacokinetics of a new alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) modulator, S18986 [(S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide], in the rat". Drug Metabolism and Disposition: the Biological Fate of Chemicals 33 (8): 1137–43. DOI:10.1124/dmd.105.004424. PMID 15860654. 
  8. ↑ Béracochéa D, Philippin JN, Meunier S, Morain P, Bernard K (July 2007). "Improvement of episodic contextual memory by S 18986 in middle-aged mice: comparison with donepezil". Psychopharmacology 193 (1): 63–73. DOI:10.1007/s00213-007-0765-4. PMID 17384936. 
  9. ↑ Marighetto A, Valerio S, Jaffard R, Mormede C, Muñoz C, Bernard K, Morain P (May 2008). "The AMPA modulator S 18986 improves declarative and working memory performances in aged mice". Behavioural Pharmacology 19 (3): 235–44. DOI:10.1097/FBP.0b013e3282feb0c1. PMID 18469541. 
  10. ↑ Kelly SJ, Bernard K, Muñoz C, Lawrence RC, Thacker J, Grillo CA, Piroli GG, Reagan LP (January 2009). "Effects of the AMPA receptor modulator S 18986 on measures of cognition and oxidative stress in aged rats". Psychopharmacology 202 (1-3): 225–35. DOI:10.1007/s00213-008-1301-x. PMID 18762915. 
  11. ↑ Gupta SK, Mishra R, Kusum S, Spedding M, Meiri KF, Gressens P, Mani S (April 2009). "GAP-43 is essential for the neurotrophic effects of BDNF and positive AMPA receptor modulator S18986". Cell Death and Differentiation 16 (4): 624–37. DOI:10.1038/cdd.2008.188. PMID 19136940. 
  12. ↑ Destot-Wong KD, Liang K, Gupta SK, Favrais G, Schwendimann L, Pansiot J, Baud O, Spedding M, Lelièvre V, Mani S, Gressens P (September 2009). "The AMPA receptor positive allosteric modulator, S18986, is neuroprotective against neonatal excitotoxic and inflammatory brain damage through BDNF synthesis". Neuropharmacology 57 (3): 277–86. DOI:10.1016/j.neuropharm.2009.05.010. PMID 19501111. 

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