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20-September-2008 09:55:56 - GTS-21 GTS-21 Systematic IUPAC name 3-3E-3-2,4-dimethoxyphenylmethylidene-5,6-dihydro-4H-pyridin-2-ylpyridine Identifiers CAS number ? ATC code ? PubChem 5310985 Chemical data Formula C19H20N2O2 Mol. mass 308.374 SMILES eMolecules PubChem Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? GTS-21 DMXB-A is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It binds to both the α4β2 and α7 subtypes, but only activates the α7 to any significant extent.12 Both GTS-21 itself and its demethylated active metabolite 4-OH-GTS-213 display nootropic4 and neuroprotective effects,5678 and GTS-21 is being investigated for the treatment of Alzheimer's disease,9 nicotine dependence,10 and most importantly for schizophrenia.1112131415 Tablets This pharmacology-related article is a stub. References ^ Briggs CA, Anderson DJ, Brioni JD, Buccafusco JJ, Buckley MJ, Campbell JE, Decker MW, Donnelly-Roberts D, Elliott RL, Gopalakrishnan M, Holladay MW, Hui YH, Jackson WJ, Kim DJ, Marsh KC, O'Neill A, Prendergast MA, Ryther KB, Sullivan JP, Arneric SP. Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacology, Biochemistry and Behaviour. 1997 May-Jun;571-2:231-41. PMID 9164577 ^ Meyer EM, Tay ET, Papke RL, Meyers C, Huang GL, de Fiebre CM. 3-2,4-Dimethoxybenzylideneanabaseine DMXB selectively activates rat alpha7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner. Brain Research. 1997 Sep 12;7681-2:49-56. PMID 9369300 ^ Meyer EM, Kuryatov A, Gerzanich V, Lindstrom J, Papke RL. Analysis of 3-4-hydroxy, 2-Methoxybenzylideneanabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors. Journal of Pharmacology and Experimental Therapeutics. 1998 Dec;2873:918-25. PMID 9864273 ^ Kitagawa H, Takenouchi T, Azuma R, Wesnes KA, Kramer WG, Clody DE, Burnett AL. Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. Neuropsychopharmacology. 2003 Mar;283:542-51. PMID 12629535 ^ Meyer EM, King MA, Meyers C. Neuroprotective effects of 2,4-dimethoxybenzylidene anabaseine DMXB and tetrahydroaminoacridine THA in neocortices of nucleus basalis lesioned rats. Brain Research. 1998 Mar 9;7861-2:252-4. PMID 9555043 ^ Shimohama S, Greenwald DL, Shafron DH, Akaika A, Maeda T, Kaneko S, Kimura J, Simpkins CE, Day AL, Meyer EM. Nicotinic alpha 7 receptors protect against glutamate neurotoxicity and neuronal ischemic damage. Brain Research. 1998 Jan 1;7791-2:359-63. PMID 9473725 ^ Li Y, Meyer EM, Walker DW, Millard WJ, He YJ, King MA. Alpha7 nicotinic receptor activation inhibits ethanol-induced mitochondrial dysfunction, cytochrome c release and neurotoxicity in primary rat hippocampal neuronal cultures. Journal of Neurochemistry. 2002 May;814:853-8. PMID 12065644 ^ de Fiebre NC, de Fiebre CM. Alpha 7 nicotinic acetylcholine receptor-mediated protection against ethanol-induced neurotoxicity. Alcohol. 2003 Nov;313:149-53. PMID 14693263 ^ Kem WR. The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA GTS-21. Behavioural Brain Research. 2000 Aug;1131-2:169-81. PMID 10942043 ^ Foulds J, Burke M, Steinberg M, Williams JM, Ziedonis DM. Advances in pharmacotherapy for tobacco dependence. Expert Opinion on Emerging Drugs. 2004 May;91:39-53. PMID 15155135 ^ Simosky JK, Stevens KE, Freedman R. Nicotinic agonists and psychosis. Current Drug Targets. CNS and Neurological Disorders. 2002 Apr;12:149-62. PMID 12769624 ^ Martin LF, Kem WR, Freedman R. Alpha-7 nicotinic receptor agonists: potential new candidates for the treatment of schizophrenia. Psychopharmacology Berlin. 2004 Jun;1741:54-64. PMID 15205879 ^ Olincy A, Harris JG, Johnson LL, Pender V, Kongs S, Allensworth D, Ellis J, Zerbe GO, Leonard S, Stevens KE, Stevens JO, Martin L, Adler LE, Soti F, Kem WR, Freedman R. Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia. Archives of General Psychiatry. 2006 Jun;636:630-8. PMID 16754836 ^ Olincy A, Stevens KE. Treating schizophrenia symptoms with an alpha7 nicotinic agonist, from mice to men. Biochemical Pharmacology. 2007 Oct 15;748:1192-201. PMID 17714692 ^ Freedman R, Olincy A, Buchanan RW, Harris JG, Gold JM, Johnson L, Allensworth D, Guzman-Bonilla A, Clement B, Ball MP, Kutnick J, Pender V, Martin LF, Stevens KE, Wagner BD, Zerbe GO, Soti F, Kem WR. Initial Phase 2 Trial of a Nicotinic Agonist in Schizophrenia. American Journal of Psychiatry. 2008 Apr 1. Epub ahead of print PMID 18381905 v d e Stimulants Alkylamines Cyclopentamine Geranamine Isometheptene Octodrine Propylhexedrine Tuamine Alphapyrrolidinylalkiophenones α-PPP MDPPP MDPV MPBP MPHP MPPP MOPPP Pyrovalerone Cholinergics ABT-089 ABT-418 Anabasine Arecoline Cotinine Cytisine Dianicline Epibatidine Epiboxidine GTS-21 Ispronicline Nicotine Rivanicline Tebanicline Varenicline Convulsants Bicuculline DMCM Gabazine Pentetrazol Picrotoxin Strychnine Thujone Eugeroics Adrafinil Armodafinil Carphedon Modafinil Phenethylamines 4-Bromomethcathinone 4-Fluoroamphetamine 4-Fluoromethamphetamine 4-Fluoromethcathinone 4-Methylmethcathinone 4-MTA Aletamine Amfepentorex Amphechloral Amphetamine Dextroamphetamine, Adderall Amphetaminil Benzphetamine Bupropion Cathinone Chlorphentermine Clenbuterol Clobenzorex Clortermine Diethylpropion Dimethoxyamphetamine Dimethylamphetamine Dimethylcathinone Ephedrine Epinephrine Ethcathinone Ethylamphetamine Fenethylline Fenfluramine Fenproporex Fludorex Furfenorex Levomethamphetamine Lisdexamfetamine MDMA Mefenorex Methamphetamine Methcathinone Methoxyphedrine Methylone Octopamine Ortetamine Parahydroxyamphetamine PCA PIA PMA PMEA PMMA PPAP Phendimetrazine Phenmetrazine Phentermine Phenylephrine Phenylpropanolamine Propylamphetamine Pseudoephedrine Selegiline Synephrine Tiflorex Xylopropamine Phenylaminooxazoles 4-Methyl-aminorex Aminorex Clominorex Fenozolone Fluminorex Pemoline Thozalinone Piperazines 2C-B-BZP BZP GBR-12783 GBR-12935 GBR-13069 GBR-13098 GBR-13119 MeOPP MBZP Vanoxerine Piperidines 2-Benzylpiperidine Desoxypipradrol Diphemethoxidine Ethylphenidate HDMP-28 --Methyl-1-methyl-4β-2-naphthylpiperidine-3β-carboxylate Methylphenidate Dexmethylphenidate Nocaine Phacetoperane Pipradrol Tropanes 3α-Bis-4-fluorophenylmethoxytropane 3α-4-Chlorophenylphenylmethoxytropane 3-Pseudotropyl-4-fluorobenzoate Altropane IACFT Brasofensine CFT WIN 35,428 β-CIT RTI-55 Cocaethylene Cocaine β-CPPIT Dichloropane RTI-111 Difluoropine FE-β-CPPIT FP-β-CPPIT PIT PTT RTI-31 RTI-32 RTI-51 RTI-112 RTI-113 RTI-121 IPCIT RTI-126 RTI-150 RTI-171 RTI-177 RTI-336 Tesofensine Troparil β-CPT, WIN 35,065-2 WF-23 WF-33 WF-60 Xanthines Aminophylline Caffeine Dimethazan Paraxanthine Theobromine Theophylline Others Amineptine Bemegride Benzydamine BPAP Bromantane BTQ Clofenciclan Cypenamine Cyprodenate Diclofensine Dimethocaine Diphenyl prolinol Ethamivan Fencamfamine Feprosidnine Gilutensin GYKI-52895 Hexacyclonate Indanorex Indatraline LR-5182 Mazindol Mesocarb Naphthylisopropylamine Nikethamide Nomifensine Phthalimidopropiophenone Prolintane Sibutramine Yohimbine Zylofuramine See also Sympathomimetic amines Retrieved from http://en..org/wiki/GTS-21 Categories: Pharmacology stubs | Antipsychotics | Pyridines | Nicotinic agonists | Stimulants Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 1 June 2008, at 23:47
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