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Items: 1 to 50 of 88

1.

Discovery and characterization of novel indole and 7-azaindole derivatives as inhibitors of β-amyloid-42 aggregation for the treatment of Alzheimer's disease.

Sreenivasachary N, Kroth H, Benderitter P, Hamel A, Varisco Y, Hickman DT, Froestl W, Pfeifer A, Muhs A.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1405-1411. doi: 10.1016/j.bmcl.2017.02.001. Epub 2017 Feb 4.

PMID:
28216401
2.

Synthesis and structure-activity relationship of 2,6-disubstituted pyridine derivatives as inhibitors of β-amyloid-42 aggregation.

Kroth H, Sreenivasachary N, Hamel A, Benderitter P, Varisco Y, Giriens V, Paganetti P, Froestl W, Pfeifer A, Muhs A.

Bioorg Med Chem Lett. 2016 Jul 15;26(14):3330-3335. doi: 10.1016/j.bmcl.2016.05.040. Epub 2016 May 13.

PMID:
27256911
3.

Cognitive enhancers (Nootropics). Part 3: drugs interacting with targets other than receptors or enzymes. Disease-modifying drugs. Update 2014.

Froestl W, Pfeifer A, Muhs A.

J Alzheimers Dis. 2014;42(4):1079-149. doi: 10.3233/JAD-141206. Review.

PMID:
25061058
4.

Cognitive enhancers (nootropics). Part 2: drugs interacting with enzymes. Update 2014.

Froestl W, Muhs A, Pfeifer A.

J Alzheimers Dis. 2014;42(1):1-68. doi: 10.3233/JAD-140402. Review.

PMID:
24903780
5.

Cognitive enhancers (Nootropics). Part 1: drugs interacting with receptors. Update 2014.

Froestl W, Muhs A, Pfeifer A.

J Alzheimers Dis. 2014;41(4):961-1019. doi: 10.3233/JAD-140228. Review.

PMID:
24898652
6.

Increased efflux of amyloid-β peptides through the blood-brain barrier by muscarinic acetylcholine receptor inhibition reduces pathological phenotypes in mouse models of brain amyloidosis.

Paganetti P, Antoniello K, Devraj K, Toni N, Kieran D, Madani R, Pihlgren M, Adolfsson O, Froestl W, Schrattenholz A, Liebner S, Havas D, Windisch M, Cirrito JR, Pfeifer A, Muhs A.

J Alzheimers Dis. 2014;38(4):767-86. doi: 10.3233/JAD-131091.

PMID:
24072071
7.

Cognitive enhancers (nootropics). Part 3: drugs interacting with targets other than receptors or enzymes. disease-modifying drugs.

Froestl W, Pfeifer A, Muhs A.

J Alzheimers Dis. 2013;34(1):1-114. doi: 10.3233/JAD-121729. Review.

PMID:
23186990
8.

Cognitive enhancers (nootropics). Part 2: drugs interacting with enzymes.

Froestl W, Muhs A, Pfeifer A.

J Alzheimers Dis. 2013;33(3):547-658. doi: 10.3233/JAD-2012-121537. Review.

PMID:
23042218
9.

Discovery and structure activity relationship of small molecule inhibitors of toxic β-amyloid-42 fibril formation.

Kroth H, Ansaloni A, Varisco Y, Jan A, Sreenivasachary N, Rezaei-Ghaleh N, Giriens V, Lohmann S, López-Deber MP, Adolfsson O, Pihlgren M, Paganetti P, Froestl W, Nagel-Steger L, Willbold D, Schrader T, Zweckstetter M, Pfeifer A, Lashuel HA, Muhs A.

J Biol Chem. 2012 Oct 5;287(41):34786-800. doi: 10.1074/jbc.M112.357665. Epub 2012 Aug 13.

10.

Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors.

Froestl W, Muhs A, Pfeifer A.

J Alzheimers Dis. 2012;32(4):793-887. doi: 10.3233/JAD-2012-121186. Review.

PMID:
22886028
11.

The development of medications for alcohol-use disorders targeting the GABAB receptor system.

Agabio R, Maccioni P, Carai MA, Gessa GL, Froestl W, Colombo G.

Recent Pat CNS Drug Discov. 2012 Aug;7(2):113-28. Review.

PMID:
22574677
12.

Activation of the GABA(B) Receptor Prevents Nicotine-Induced Locomotor Stimulation in Mice.

Lobina C, Carai MA, Froestl W, Mugnaini C, Pasquini S, Corelli F, Gessa GL, Colombo G.

Front Psychiatry. 2011 Dec 30;2:76. doi: 10.3389/fpsyt.2011.00076. eCollection 2011.

13.

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, Urwyler S.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):996-9. doi: 10.1016/j.bmcl.2011.12.009. Epub 2011 Dec 8.

PMID:
22197388
14.

An historical perspective on GABAergic drugs.

Froestl W.

Future Med Chem. 2011 Feb;3(2):163-75. doi: 10.4155/fmc.10.285.

PMID:
21428811
15.

The GABA B receptor agonist CGP44532 and the positive modulator GS39783 reverse some behavioural changes related to positive syndromes of psychosis in mice.

Wierońska JM, Kusek M, Tokarski K, Wabno J, Froestl W, Pilc A.

Br J Pharmacol. 2011 Jul;163(5):1034-47. doi: 10.1111/j.1476-5381.2011.01301.x.

16.

Both GABA(B) receptor activation and blockade exacerbated anhedonic aspects of nicotine withdrawal in rats.

Vlachou S, Paterson NE, Guery S, Kaupmann K, Froestl W, Banerjee D, Finn MG, Markou A.

Eur J Pharmacol. 2011 Mar 25;655(1-3):52-8. doi: 10.1016/j.ejphar.2011.01.009. Epub 2011 Jan 22.

17.

Repeated administration of the GABAB receptor positive modulator BHF177 decreased nicotine self-administration, and acute administration decreased cue-induced reinstatement of nicotine seeking in rats.

Vlachou S, Guery S, Froestl W, Banerjee D, Benedict J, Finn MG, Markou A.

Psychopharmacology (Berl). 2011 May;215(1):117-28. doi: 10.1007/s00213-010-2119-x. Epub 2010 Dec 22.

18.

Chemistry and pharmacology of GABAB receptor ligands.

Froestl W.

Adv Pharmacol. 2010;58:19-62. doi: 10.1016/S1054-3589(10)58002-5.

PMID:
20655477
19.

Novel GABA(B) receptor positive modulators: a patent survey.

Froestl W.

Expert Opin Ther Pat. 2010 Aug;20(8):1007-17. doi: 10.1517/13543776.2010.506480. Review.

PMID:
20645682
20.

Reduction of alcohol's reinforcing and motivational properties by the positive allosteric modulator of the GABA(B) receptor, BHF177, in alcohol-preferring rats.

Maccioni P, Carai MA, Kaupmann K, Guery S, Froestl W, Leite-Morris KA, Gessa GL, Colombo G.

Alcohol Clin Exp Res. 2009 Oct;33(10):1749-56. doi: 10.1111/j.1530-0277.2009.01012.x. Epub 2009 Jul 1.

PMID:
19572981
21.

Specific reduction of alcohol's motivational properties by the positive allosteric modulator of the GABAB receptor, GS39783--comparison with the effect of the GABAB receptor direct agonist, baclofen.

Maccioni P, Fantini N, Froestl W, Carai MA, Gessa GL, Colombo G.

Alcohol Clin Exp Res. 2008 Sep;32(9):1558-64. doi: 10.1111/j.1530-0277.2008.00725.x. Epub 2008 Jul 9.

PMID:
18616673
22.

Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats.

Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A.

J Pharmacol Exp Ther. 2008 Jul;326(1):306-14. doi: 10.1124/jpet.108.139204. Epub 2008 Apr 29.

23.

Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.

Guery S, Floersheim P, Kaupmann K, Froestl W.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6206-11. Epub 2007 Sep 8.

24.

Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats.

Maccioni P, Pes D, Orrù A, Froestl W, Gessa GL, Carai MA, Colombo G.

Psychopharmacology (Berl). 2007 Aug;193(2):171-8. Epub 2007 Mar 29.

PMID:
17393141
25.

Attenuation of cocaine-seeking by GABA B receptor agonists baclofen and CGP44532 but not the GABA reuptake inhibitor tiagabine in baboons.

Weerts EM, Froestl W, Kaminski BJ, Griffiths RR.

Drug Alcohol Depend. 2007 Jul 10;89(2-3):206-13. Epub 2007 Jan 16.

26.

Chronic intragastric administration of gamma-butyrolactone produces physical dependence in baboons.

Goodwin AK, Griffiths RR, Brown PR, Froestl W, Jakobs C, Gibson KM, Weerts EM.

Psychopharmacology (Berl). 2006 Nov;189(1):71-82. Epub 2006 Sep 20.

PMID:
17047936
27.

Antidepressant-like activity of CGP 36742 and CGP 51176, selective GABAB receptor antagonists, in rodents.

Nowak G, Partyka A, Pałucha A, Szewczyk B, Wierońska JM, Dybała M, Metz M, Librowski T, Froestl W, Papp M, Pilc A.

Br J Pharmacol. 2006 Nov;149(5):581-90. Epub 2006 Aug 21.

28.

Influence of a GABA(B) and GABA(C) receptor antagonist on sleep-waking cycle in the rat.

Deschaux O, Froestl W, Gottesmann C.

Eur J Pharmacol. 2006 Mar 27;535(1-3):177-81. Epub 2006 Mar 15.

PMID:
16540106
29.

Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats.

Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, Froestl W, Gessa GL, Carai MA, Colombo G.

Eur J Pharmacol. 2005 Nov 21;525(1-3):105-11. Epub 2005 Nov 14.

PMID:
16289452
30.

Effects of GABAergic modulators on food and cocaine self-administration in baboons.

Weerts EM, Froestl W, Griffiths RR.

Drug Alcohol Depend. 2005 Dec 12;80(3):369-76. Epub 2005 Jul 7.

PMID:
16005580
31.

Prolonged nicotine exposure does not alter GABA(B) receptor-mediated regulation of brain reward function.

Paterson NE, Bruijnzeel AW, Kenny PJ, Wright CD, Froestl W, Markou A.

Neuropharmacology. 2005 Dec;49(7):953-62. Epub 2005 Jul 7.

PMID:
16005474
33.

Involvement of gamma-hydroxybutyrate (GHB) and GABA-B receptors in the acute behavioral effects of GHB in baboons.

Goodwin AK, Froestl W, Weerts EM.

Psychopharmacology (Berl). 2005 Jul;180(2):342-51. Epub 2005 Mar 1.

PMID:
15739078
34.

Spontaneous and precipitated withdrawal after chronic intragastric administration of gamma-hydroxybutyrate (GHB) in baboons.

Weerts EM, Goodwin AK, Griffiths RR, Brown PR, Froestl W, Jakobs C, Gibson KM.

Psychopharmacology (Berl). 2005 May;179(3):678-87. Epub 2005 Jan 12.

PMID:
15645222
35.

In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor.

Carai MA, Colombo G, Froestl W, Gessa GL.

Eur J Pharmacol. 2004 Nov 19;504(3):213-6.

PMID:
15541424
36.

Determination of the minimal functional ligand-binding domain of the GABAB1b receptor.

Deriu D, Gassmann M, Firbank S, Ristig D, Lampert C, Mosbacher J, Froestl W, Kaupmann K, Bettler B, Grütter MG.

Biochem J. 2005 Mar 15;386(Pt 3):423-31.

37.

SGS742: the first GABA(B) receptor antagonist in clinical trials.

Froestl W, Gallagher M, Jenkins H, Madrid A, Melcher T, Teichman S, Mondadori CG, Pearlman R.

Biochem Pharmacol. 2004 Oct 15;68(8):1479-87.

PMID:
15451390
39.

Redistribution of GABAB(1) protein and atypical GABAB responses in GABAB(2)-deficient mice.

Gassmann M, Shaban H, Vigot R, Sansig G, Haller C, Barbieri S, Humeau Y, Schuler V, Müller M, Kinzel B, Klebs K, Schmutz M, Froestl W, Heid J, Kelly PH, Gentry C, Jaton AL, Van der Putten H, Mombereau C, Lecourtier L, Mosbacher J, Cryan JF, Fritschy JM, Lüthi A, Kaupmann K, Bettler B.

J Neurosci. 2004 Jul 7;24(27):6086-97.

40.

GABAB receptors in Schwann cells influence proliferation and myelin protein expression.

Magnaghi V, Ballabio M, Cavarretta IT, Froestl W, Lambert JJ, Zucchi I, Melcangi RC.

Eur J Neurosci. 2004 May;19(10):2641-9.

PMID:
15147298
41.

Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines.

Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, Froestl W, Bettler B, Kaupmann K, Spooren WP.

J Pharmacol Exp Ther. 2004 Sep;310(3):952-63. Epub 2004 Apr 27.

PMID:
15113848
42.

Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior.

Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF.

Neuropsychopharmacology. 2004 Jun;29(6):1050-62.

43.

Suppression of GABA(B) receptor function in vivo by disulfide reducing agent, DL-dithiothreitol (DTT).

Carai MA, Vacca G, Serra S, Colombo G, Froestl W, Gessa GL.

Psychopharmacology (Berl). 2004 Jul;174(2):283-90.

PMID:
14760512
44.

Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats.

Smith MA, Yancey DL, Morgan D, Liu Y, Froestl W, Roberts DC.

Psychopharmacology (Berl). 2004 Apr;173(1-2):105-11. Epub 2004 Jan 8.

PMID:
14712341
45.

Specific gamma-hydroxybutyrate-binding sites but loss of pharmacological effects of gamma-hydroxybutyrate in GABA(B)(1)-deficient mice.

Kaupmann K, Cryan JF, Wellendorph P, Mombereau C, Sansig G, Klebs K, Schmutz M, Froestl W, van der Putten H, Mosbacher J, Bräuner-Osborne H, Waldmeier P, Bettler B.

Eur J Neurosci. 2003 Nov;18(10):2722-30.

PMID:
14656321
46.

The GABAB receptor agonists baclofen and CGP44532 decreased nicotine self-administration in the rat.

Paterson NE, Froestl W, Markou A.

Psychopharmacology (Berl). 2004 Mar;172(2):179-86. Epub 2003 Nov 11.

PMID:
14610636
47.

N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function.

Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K.

J Pharmacol Exp Ther. 2003 Oct;307(1):322-30. Epub 2003 Sep 3.

PMID:
12954816
48.

Ligands for expression cloning and isolation of GABA(B) receptors.

Froestl W, Bettler B, Bittiger H, Heid J, Kaupmann K, Mickel SJ, Strub D.

Farmaco. 2003 Mar;58(3):173-83. Review.

PMID:
12620413
49.

The GABA(B) receptor agonists baclofen and CGP 44532 prevent acquisition of alcohol drinking behaviour in alcohol-preferring rats.

Colombo G, Serra S, Brunetti G, Atzori G, Pani M, Vacca G, Addolorato G, Froestl W, Carai MA, Gessa GL.

Alcohol Alcohol. 2002 Sep-Oct;37(5):499-503.

PMID:
12217946
50.

Focal neurometabolic alterations in mice deficient for succinate semialdehyde dehydrogenase.

Gibson KM, Schor DS, Gupta M, Guerand WS, Senephansiri H, Burlingame TG, Bartels H, Hogema BM, Bottiglieri T, Froestl W, Snead OC, Grompe M, Jakobs C.

J Neurochem. 2002 Apr;81(1):71-9.

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