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225 related items for PubMed ID: 16220991

  • 1. A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents.
    Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, Gratteri P, Besnard F, Costa B, Montali M, Martini C, Fohlin J, De Siena G, Aiello PM.
    J Med Chem; 2005 Oct 20; 48(21):6756-60. PubMed ID: 16220991
    [Abstract] [Full Text] [Related]

  • 2. Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.
    Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, Gratteri P, Bonaccini C, Malmberg Aiello P, Besnard F, Renard S, Costa B, Martini C.
    J Med Chem; 2003 Jan 16; 46(2):310-3. PubMed ID: 12519068
    [Abstract] [Full Text] [Related]

  • 3. The anxioselective agent 7-(2-chloropyridin-4-yl)pyrazolo-[1,5-a]-pyrimidin-3-yl](pyridin-2-yl)methanone (DOV 51892) is more efficacious than diazepam at enhancing GABA-gated currents at alpha1 subunit-containing GABAA receptors.
    Popik P, Kostakis E, Krawczyk M, Nowak G, Szewczyk B, Krieter P, Chen Z, Russek SJ, Gibbs TT, Farb DH, Skolnick P, Lippa AS, Basile AS.
    J Pharmacol Exp Ther; 2006 Dec 16; 319(3):1244-52. PubMed ID: 16971504
    [Abstract] [Full Text] [Related]

  • 4. Benzodiazepine receptor ligands. 8: synthesis and pharmacological evaluation of new pyrazolo[5,1-c] [1,2,4]benzotriazine 5-oxide 3- and 8-disubstituted: high affinity ligands endowed with inverse-agonist pharmacological efficacy.
    Guerrini G, Costanzo A, Ciciani G, Bruni F, Selleri S, Costagli C, Besnard F, Costa B, Martini C, De Siena G, Malmberg-Aiello P.
    Bioorg Med Chem; 2006 Feb 01; 14(3):758-75. PubMed ID: 16214350
    [Abstract] [Full Text] [Related]

  • 5. Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.
    McKernan RM, Rosahl TW, Reynolds DS, Sur C, Wafford KA, Atack JR, Farrar S, Myers J, Cook G, Ferris P, Garrett L, Bristow L, Marshall G, Macaulay A, Brown N, Howell O, Moore KW, Carling RW, Street LJ, Castro JL, Ragan CI, Dawson GR, Whiting PJ.
    Nat Neurosci; 2000 Jun 01; 3(6):587-92. PubMed ID: 10816315
    [Abstract] [Full Text] [Related]

  • 6. Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors.
    Cox ED, Diaz-Arauzo H, Huang Q, Reddy MS, Ma C, Harris B, McKernan R, Skolnick P, Cook JM.
    J Med Chem; 1998 Jul 02; 41(14):2537-52. PubMed ID: 9651158
    [Abstract] [Full Text] [Related]

  • 7. RP 59037 and RP 60503: anxiolytic cyclopyrrolone derivatives with low sedative potential. interaction with the gamma-aminobutyric acidA/benzodiazepine receptor complex and behavioral effects in the rodent.
    Doble A, Canton T, Dreisler S, Piot O, Boireau A, Stutzmann JM, Bardone MC, Rataud J, Roux M, Roussel G.
    J Pharmacol Exp Ther; 1993 Sep 02; 266(3):1213-26. PubMed ID: 8103792
    [Abstract] [Full Text] [Related]

  • 8. 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
    Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ.
    J Med Chem; 2005 Nov 17; 48(23):7089-92. PubMed ID: 16279764
    [Abstract] [Full Text] [Related]

  • 9. New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
    Jurczyk S, Kołaczkowski M, Maryniak E, Zajdel P, Pawłowski M, Tatarczyńska E, Kłodzińska A, Chojnacka-Wójcik E, Bojarski AJ, Charakchieva-Minol S, Duszyńska B, Nowak G, Maciag D.
    J Med Chem; 2004 May 06; 47(10):2659-66. PubMed ID: 15115407
    [Abstract] [Full Text] [Related]

  • 10. Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
    Primofiore G, Taliani S, Da Settimo F, Marini AM, La Motta C, Simorini F, Patrizi MP, Sergianni V, Novellino E, Greco G, Cosimelli B, Calderone V, Montali M, Besnard F, Martini C.
    J Med Chem; 2007 Apr 05; 50(7):1627-34. PubMed ID: 17335185
    [Abstract] [Full Text] [Related]

  • 11. GABA A receptor subtype selectivity underlying selective anxiolytic effect of baicalin.
    Wang F, Xu Z, Ren L, Tsang SY, Xue H.
    Neuropharmacology; 2008 Dec 05; 55(7):1231-7. PubMed ID: 18723037
    [Abstract] [Full Text] [Related]

  • 12. GABAA receptor pharmacology of fluorinated derivatives of the novel sedative-hypnotic pyrazolopyrimidine indiplon.
    Wegner F, Deuther-Conrad W, Scheunemann M, Brust P, Fischer S, Hiller A, Diekers M, Strecker K, Wohlfarth K, Allgaier C, Steinbach J, Hoepping A.
    Eur J Pharmacol; 2008 Feb 02; 580(1-2):1-11. PubMed ID: 18035350
    [Abstract] [Full Text] [Related]

  • 13. 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
    Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL.
    J Med Chem; 2004 Mar 25; 47(7):1807-22. PubMed ID: 15027873
    [Abstract] [Full Text] [Related]

  • 14. CNS 7056: a novel ultra-short-acting Benzodiazepine.
    Kilpatrick GJ, McIntyre MS, Cox RF, Stafford JA, Pacofsky GJ, Lovell GG, Wiard RP, Feldman PL, Collins H, Waszczak BL, Tilbrook GS.
    Anesthesiology; 2007 Jul 25; 107(1):60-6. PubMed ID: 17585216
    [Abstract] [Full Text] [Related]

  • 15. New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling investigation.
    Guerrini G, Ciciani G, Bruni F, Selleri S, Guarino C, Melani F, Montali M, Daniele S, Martini C, Ghelardini C, Norcini M, Ciattini S, Costanzo A.
    J Med Chem; 2010 Nov 11; 53(21):7532-48. PubMed ID: 20939501
    [Abstract] [Full Text] [Related]

  • 16. TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates.
    Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, Ragan I, Kerby J, Street L, Carling R, Castro JL, Whiting P, Dawson GR, McKernan RM.
    J Pharmacol Exp Ther; 2006 Jan 11; 316(1):410-22. PubMed ID: 16183706
    [Abstract] [Full Text] [Related]

  • 17. A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
    Lewis RT, Blackaby WP, Blackburn T, Jennings AS, Pike A, Wilson RA, Hallett DJ, Cook SM, Ferris P, Marshall GR, Reynolds DS, Sheppard WF, Smith AJ, Sohal B, Stanley J, Tye SJ, Wafford KA, Atack JR.
    J Med Chem; 2006 Apr 20; 49(8):2600-10. PubMed ID: 16610803
    [Abstract] [Full Text] [Related]

  • 18. Pyrazolo[4,3-c]quinolines, synthesis and specific inhibition of benzodiazepine receptor binding. Note II.
    Savini L, Massarelli P, Corti P, Pellerano C, Bruni G, Romeo MR.
    Farmaco; 1993 Dec 20; 48(12):1675-86. PubMed ID: 8135991
    [Abstract] [Full Text] [Related]

  • 19. Selective anxiolytics: are the actions related to partial "agonist" activity or a preferential affinity for benzodiazepine receptor subtypes?
    Gee KW, Yamamura HI.
    Adv Biochem Psychopharmacol; 1983 Dec 20; 38():1-9. PubMed ID: 6142598
    [Abstract] [Full Text] [Related]

  • 20. High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
    Primofiore G, Da Settimo F, Taliani S, Salerno S, Novellino E, Greco G, Cosimelli B, Besnard F, Costa B, Montali M, Martini C.
    J Med Chem; 2005 Apr 21; 48(8):2936-43. PubMed ID: 15828832
    [Abstract] [Full Text] [Related]

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