S-18986

化合物

S-18986,是一种与环噻嗪相关的AMPA受体正变构调节剂。动物研究發現S-18986有促智神经保护的作用,另外這種物質能誘導大脑海馬體额叶皮层脑源性神经营养因子α-氨基-3-羥基-5-甲基-4-異惡唑丙酸(AMPA)介导去甲肾上腺素乙酰胆碱释放。[1][2][3][4][5][6][7][8][9][10]

S-18986
法律規範狀態
法律規範
  • Investigational New Drug
识别信息
  • (S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide
CAS号175340-20-2  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C10H12N2O2S
摩尔质量224.28 g·mol−1
3D模型(JSmol英语JSmol
  • C1C[C@@H]2NS(=O)(=O)C3=CC=CC=C3N2C1
  • InChI=1S/C10H12N2O2S/c13-15(14)9-5-2-1-4-8(9)12-7-3-6-10(12)11-15/h1-2,4-5,10-11H,3,6-7H2/t10-/m1/s1 ☒N
  • Key:MNTIJYGEITVWHU-SNVBAGLBSA-N ☒N

參見

参考文獻

  1. ^ (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. August 2000, 401 (2): 145–53. PMID 10924919. doi:10.1016/S0014-2999(00)00433-7. 
  2. ^ Effects of S 18986-1, a novel cognitive enhancer, on memory performances in an object recognition task in rats. European Journal of Pharmacology. August 2000, 401 (2): 205–12. PMID 10924928. doi:10.1016/S0014-2999(00)00429-5. 
  3. ^ Positive allosteric modulators of AMPA receptors are neuroprotective against lesions induced by an NMDA agonist in neonatal mouse brain. Brain Research. April 2003, 970 (1–2): 221–5. PMID 12706264. doi:10.1016/S0006-8993(03)02357-6. 
  4. ^ 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. May 2004, 361 (1–3): 120–3. PMID 15135908. doi:10.1016/j.neulet.2003.12.061. 
  5. ^ 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. August 2005, 33 (8): 1137–43. PMID 15860654. doi:10.1124/dmd.105.004424. 
  6. ^ Improvement of episodic contextual memory by S 18986 in middle-aged mice: comparison with donepezil. Psychopharmacology. July 2007, 193 (1): 63–73. PMID 17384936. doi:10.1007/s00213-007-0765-4. 
  7. ^ The AMPA modulator S 18986 improves declarative and working memory performances in aged mice. Behavioural Pharmacology. May 2008, 19 (3): 235–44. PMID 18469541. doi:10.1097/FBP.0b013e3282feb0c1. 
  8. ^ Effects of the AMPA receptor modulator S 18986 on measures of cognition and oxidative stress in aged rats. Psychopharmacology. January 2009, 202 (1–3): 225–35. PMID 18762915. doi:10.1007/s00213-008-1301-x. 
  9. ^ GAP-43 is essential for the neurotrophic effects of BDNF and positive AMPA receptor modulator S18986. Cell Death and Differentiation. April 2009, 16 (4): 624–37. PMID 19136940. doi:10.1038/cdd.2008.188. 
  10. ^ The AMPA receptor positive allosteric modulator, S18986, is neuroprotective against neonatal excitotoxic and inflammatory brain damage through BDNF synthesis. Neuropharmacology. September 2009, 57 (3): 277–86. PMID 19501111. doi:10.1016/j.neuropharm.2009.05.010.