S-18986

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	637863
Hemijski podaci
Formula	C10H12N2O2S
Mol. masa	224,279 g/mol
SMILES	eMolekuli & PubHem
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
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

↑ 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. edit
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.

Povezano

IDRA-21

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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. 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.

[pmid10924919-3] 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.

[pmid10924928-4] 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.

[pmid12706264-5] 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.

[pmid15135908-6] 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.

[pmid15860654-7] 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.

[pmid17384936-8] 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.

[pmid18469541-9] 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.

[pmid18762915-10] 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.

[pmid19136940-11] 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.

[pmid19501111-12] 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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