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16-September-2008 16:15:12 - ABT-239 ABT-239 Systematic IUPAC name 4-2-2-2R-2-Methylpyrrolidin-1-ylethyl- benzofuran-5-ylbenzonitrile Identifiers CAS number ? ATC code ? PubChem 9818903 Chemical data Formula C22H22N2O Mol. mass 330.42 g/mol SMILES eMolecules PubChem Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and is currently being investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia.1234 ABT-239 is more active at the human H3 receptor than comparable agents such as thioperamide, ciproxifan, and cipralisant. References ^ Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, Marsh K, Bennani YL, Cowart MD, Sullivan JP, Hancock AA 2005. Pharmacological properties of ABT-239 4-2-2-2R-2-Methylpyrrolidinylethyl-benzofuran-5-ylbenzonitrile: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J. Pharmacol. Exp. Ther. 313 1: 165-75. doi:10.1124/jpet.104.078303. PMID 15608078. ^ Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan JP, Cowart MD, Decker MW, Hancock AA 2005. Pharmacological properties of ABT-239 4-2-2-2R-2-Methylpyrrolidinylethyl-benzofuran-5-ylbenzonitrile: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J. Pharmacol. Exp. Ther. 313 1: 176-90. doi:10.1124/jpet.104.078402. PMID 15608077. ^ Cowart M, Faghih R, Curtis MP, Gfesser GA, Bennani YL, Black LA, Pan L, Marsh KC, Sullivan JP, Esbenshade TA, Fox GB, Hancock AA 2005. 4-2-2-2R-methylpyrrolidin-1-ylethylbenzofuran-5-ylbenzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. J. Med. Chem. 48 1: 38-55. doi:10.1021/jm040118g. PMID 15634000. ^ Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H June 2008. Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists. J. Pharmacol. Exp. Ther. 325 3: 902-9. doi:10.1124/jpet.107.135343. PMID 18305012. External links MeSH 4-2-2-2-methyl-1-pyrrolidinylethyl-1-benzofuran-5-ylbenzonitrile Tablets This pharmacology-related article is a stub. v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 v d e Psychoanaleptics: psychostimulants, agents used for ADHD and nootropics N06B Centrally acting sympathomimetics Amphetamine - Amphetaminil - Atomoxetine - Dextroamphetamine - Dextromethamphetamine - Fencamfamin - Fenozolone - Fenetylline - Methylphenidate - Mesocarb - Pemoline - Pipradrol - Prolintane Xanthine derivatives Caffeine - Propentofylline Glutamate receptor Racetams Aniracetam - Nefiracetam - Oxiracetam - Phenylpiracetam - Piracetam - Pramiracetam Ampakines CX-516 - CX-546 - CX-614 - CX-691 - CX-717 - IDRA-21 - LY-503,430 - PEPA Eugeroics / Benzhydryl compounds Adrafinil - Armodafinil - Modafinil Histamine H3 receptor antagonists ABT-239 - Ciproxifan Other psychostimulants and nootropics Acetylcarnitine - Citicoline - Cyprodenate - Idebenone - Ispronicline - Deanol - Dimebon - Fipexide - Linopirdine - Meclofenoxate - Nizofenone - Pirisudanol - Pyritinol - Sulbutiamine - Taltirelin - Tricyanoaminopropene - Vinpocetine Retrieved from http://en..org/wiki/ABT-239 Categories: Pharmacology stubs | Nootropics | H3 receptor antagonists 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 2 August 2008, at 05:20
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