- Improvement in the selectivity and metabolic stability of the serotonin 5-HT1A ligand, S 15535: A series of cis- and trans-2-(arylcycloalkylamine) 1-indanols
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S 15535 (1) displays a distinctive profile of agonist and antagonist (weak partial agonist) activity at pre- and postsynaptic 5-HT1A receptors, respectively. It has proven to be active in several models predictive of anxiolytic, antidepressant,
- Peglion,Goument,Despaux,Charlot,Giraud,Nisole,Newman-Tancredi,Dekeyne,Bertrand,Genissel,Millan
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p. 165 - 176
(2007/10/03)
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- 8-Methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines : Highly potent in vivo AMPA antagonists
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A novel series of readily water soluble 8-methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines were synthesized. The -10-yl acetic acid ((+)-3) and -10-carboxylidene (4) derivatives exhibit potent affinities (IC50 = 4 and 19 nM, respectively) and antagonist properties (IC50 = 2 and 3 nM, respectively) at the ionotropic AMPA receptor. These compounds also display anticonvulsant properties against both electrically and sound-induced convulsions in mice after ip, sc and iv administration with ED50 values between 0.9 and 11 mg/kg, thus suggesting adequate brain penetration. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Mignani, Serge,Bohme, Georg Andrees,Boireau, Alain,Cheve, Michel,Damour, Dominique,Debono, Marc-Williams,Genevois-Borella, Arielle,Imperato, Assunta,Jimonet, Patrick,Pratt, Jeremy,Randle, John C.R.,Ribeill, Yves,Vuilhorgne, Marc,Stutzmann, Jean-Marie
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p. 591 - 596
(2007/10/03)
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- SCHWEFELVERBINDUNGEN DES ERDOELS XXII. ALKYL-10,11-DIHYDRODIINDENOTHIOPHENE
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The one-pot syntheses of alkyl-10,11-dihydrodiindenothiophenes (3) by bromination and sulfurization of alkylindan-1-ones without substituents at C-2 (1) has been studied with 14 1 with C1-C4-rests at the benzene and or the cyclopentane ring. 9 dialkyl-3 and 3 tetraalkyl-3 are prepared in yields of 7-66percent; an octamethyl-3 is detected by tlc and ms. 2 dialkyl-3 are prepared too by an independent syntheses from dimethyl 2,5-bis(methylphenyl)thiophene-3,4-dicarboxylates (13).The mechanism of the one-pot syntheses, which gives diindeno-1,4-dithiines too,is discussed.The oxidation of 4 3 has been studied.Key words: Alkylindan-1-ones, alkyl-10,11-dihydrodiindenothiophenes, alkyldiindeno-1,4-dithiines, one-pot syntheses of anellated thiophenes, oxidation of anellated thiophenes.
- Boberg, Friedrich,Deters, Karin,Schulz, Juergen,Torges, Karl-Franz
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