S-18986 is an ampakine drug related to cyclothiazide. It has nootropic and neuroprotective effects in animal studies, and induces both production of BDNF and AMPA-mediated release of noradrenaline and acetylcholine in the hippocampus and frontal cortex of the brain.[1][2][3][4][5][6][7][8][9][10]
[edit] See also
[edit] References
- ^ 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.
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- Agonists: Glutamate/acite site competitive agonists: Aspartate
- Glutamate
- Homoquinolinic acid
- Ibotenic acid
- NMDA
- Quinolinic acid
- Tetrazolylglycine; Glycine site agonists: ACBD
- ACPC
- ACPD
- Alanine
- CCG
- Cycloserine
- DHPG
- Fluoroalanine
- Glycine
- HA-966
- L-687,414
- Milacemide
- Sarcosine
- Serine
- Tetrazolylglycine; Polyamine site agonists: Acamprosate
- Spermidine
- Spermine
Antagonists: Competitive antagonists: AP5 (APV)
- AP7
- CGP-37849
- CGP-39551
- CGP-39653
- CGP-40116
- CGS-19755
- CPP
- LY-233,053
- LY-235,959
- LY-274,614
- MDL-100,453
- Midafotel (d-CPPene)
- NPC-12,626
- NPC-17,742
- PBPD
- PEAQX
- Perzinfotel
- PPDA
- SDZ-220581
- Selfotel; Noncompetitive antagonists: ARR-15,896
- Caroverine
- Dexanabinol
- FPL-12495
- FR-115,427
- Hodgkinsine
- Magnesium
- MDL-27,266
- NPS-1506
- Psychotridine
- Zinc; Uncompetitive pore blockers: 2-MDP
- 3-MeO-PCP
- 8A-PDHQ
- Alaproclate
- Amantadine
- Aptiganel
- ARL-12,495
- ARL-15,896-AR
- ARL-16,247
- Budipine
- Delucemine
- Dexoxadrol
- Dextrallorphan
- Dieticyclidine
- Dizocilpine
- Endopsychosin
- Esketamine
- Etoxadrol
- Eticyclidine
- Gacyclidine
- Ibogaine
- Indantadol
- Ketamine
- Ketobemidone
- Loperamide
- Memantine
- Meperidine (Pethidine)
- Methadone (Levomethadone)
- Methorphan (Dextromethorphan
- Levomethorphan)
- Methoxetamine
- Milnacipran
- Morphanol (Dextrorphan
- Levorphanol)
- NEFA
- Neramexane
- Nitrous oxide
- Noribogaine
- Orphenadrine
- PCPr
- Phencyclamine
- Phencyclidine
- Propoxyphene
- Remacemide
- Rhynchophylline
- Riluzole
- Rimantadine
- Rolicyclidine
- Sabeluzole
- Tenocyclidine
- Tiletamine
- Tramadol
- Xenon; Glycine site antagonists: ACEA-1021
- ACEA-1328
- ACPC
- Carisoprodol
- CGP-39653
- CKA
- DCKA
- Felbamate
- Gavestinel
- GV-196,771
- Kynurenic acid
- L-689,560
- L-701,324
- Lacosamide
- Licostinel
- LU-73,068
- MDL-105,519
- Meprobamate
- MRZ 2/576
- PNQX
- ZD-9379; NR2B subunit antagonists: Besonprodil
- CO-101,244 (PD-174,494)
- CP-101,606
- Eliprodil
- Haloperidol
- Ifenprodil
- Isoxsuprine
- Nylidrin
- Ro8-4304
- Ro25-6981
- Traxoprodil; Polyamine site antagonists: Arcaine
- Co 101676
- Diaminopropane
- Acamprosate
- Diethylenetriamine
- Huperzine A
- Putrescine
- Ro 25-6981; Unclassified/unsorted antagonists: Chloroform
- Diethyl ether
- Enflurane
- Ethanol (Alcohol)
- Halothane
- Isoflurane
- Methoxyflurane
- Toluene
- Trichloroethane
- Trichloroethanol
- Trichloroethylene
- Xylene
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