S-18986

S-18986
法律规范状态
法律规范	美：Investigational New Drug;
识别信息
	IUPAC命名法 (S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide; ;
CAS号	175340-20-2
PubChem CID	637863;
IUPHAR/BPS	4304;
ChemSpider	553445 ;
UNII	IA262432Y9;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID40938656 ;
化学信息
化学式	C10H12N2O2S
摩尔质量	224.28 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES C1C[C@@H]2NS(=O)(=O)C3=CC=CC=C3N2C1;
	InChI 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 ; Key:MNTIJYGEITVWHU-SNVBAGLBSA-N ;

S-18986，是一种与环噻嗪相关的AMPA受体正变构调节剂。动物研究发现S-18986有促智和神经保护的作用，另外这种物质能诱导大脑海马体及额叶皮层中脑源性神经营养因子和α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）介导去甲肾上腺素及乙酰胆碱释放。^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]^[9]^[10]

参见

AMPA受体正变构调节剂

参考文献

^ (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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.

[pmid10924919-1] (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.

[pmid10924928-2] 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.

[pmid12706264-3] 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.

[pmid15135908-4] 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.

[pmid15860654-5] 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.

[pmid17384936-6] 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.

[pmid18469541-7] 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.

[pmid18762915-8] 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.

[pmid19136940-9] 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.

[pmid19501111-10] 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.

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