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.[1][2][3][4][5][6][7][8][9][10]

S-18986
IUPAC ime
(S)-2,3-dihidro-[3,4]ciklopentano-1,2,4-benzotiadiazin-1,1-dioksid
Pravni status
Pravni status
  • Novi lek u ispitivanju
Identifikatori
ATC kodnone
PubChemCID 637863
Hemijski podaci
FormulaC10H12N2O2S
Molarna masa224,279 g/mol
  • C1C[C@@H]2NS(=O)(=O)C3=CC=CC=C3N2C1

Reference уреди

  1. ^ Lockhart B, Iop F, Closier M, Lestage P (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. PMID 10924919. doi:10.1016/S0014-2999(00)00433-7. 
  2. ^ Lebrun C, Pillière E, Lestage P (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. PMID 10924928. doi:10.1016/S0014-2999(00)00429-5. 
  3. ^ Dicou E, Rangon CM, Guimiot F, Spedding M, Gressens P (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. PMID 12706264. doi:10.1016/S0006-8993(03)02357-6. 
  4. ^ Rosi S, Giovannini MG, Lestage PJ, Muñoz C, Corte LD, Pepeu G (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. PMID 15135908. doi:10.1016/j.neulet.2003.12.061. 
  5. ^ Bourasset F, Bernard K, Muñoz C, Genissel P, Scherrmann JM (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. PMID 15860654. doi:10.1124/dmd.105.004424. 
  6. ^ Béracochéa D, Philippin JN, Meunier S, Morain P, Bernard K (2007). „Improvement of episodic contextual memory by S 18986 in middle-aged mice: comparison with donepezil”. Psychopharmacology. 193 (1): 63—73. PMID 17384936. doi:10.1007/s00213-007-0765-4. 
  7. ^ Marighetto A, Valerio S, Jaffard R, Mormede C, Muñoz C, Bernard K, Morain P (2008). „The AMPA modulator S 18986 improves declarative and working memory performances in aged mice”. Behavioural Pharmacology. 19 (3): 235—44. PMID 18469541. doi:10.1097/FBP.0b013e3282feb0c1. 
  8. ^ Kelly SJ, Bernard K, Muñoz C, Lawrence RC, Thacker J, Grillo CA, Piroli GG, Reagan LP (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. PMID 18762915. doi:10.1007/s00213-008-1301-x. 
  9. ^ Gupta SK, Mishra R, Kusum S, Spedding M, Meiri KF, Gressens P, Mani S (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. PMID 19136940. doi:10.1038/cdd.2008.188. 
  10. ^ Destot-Wong KD, Liang K, Gupta SK, Favrais G, Schwendimann L, Pansiot J, Baud O, Spedding M, Lelièvre V, Mani S, Gressens P (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. PMID 19501111. doi:10.1016/j.neuropharm.2009.05.010. 

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