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Items: 1 to 50 of 53

1.

Enhanced Dendritic Inhibition and Impaired NMDAR Activation in a Mouse Model of Down Syndrome.

Schulz JM, Knoflach F, Hernandez MC, Bischofberger J.

J Neurosci. 2019 Jun 26;39(26):5210-5221. doi: 10.1523/JNEUROSCI.2723-18.2019. Epub 2019 Apr 18.

PMID:
31000585
2.

Parvalbumin expression and gamma oscillation occurrence increase over time in a neurodevelopmental model of NMDA receptor dysfunction.

van Lier B, Hierlemann A, Knoflach F.

PeerJ. 2018 Sep 19;6:e5543. doi: 10.7717/peerj.5543. eCollection 2018.

3.

Dendrite-targeting interneurons control synaptic NMDA-receptor activation via nonlinear α5-GABAA receptors.

Schulz JM, Knoflach F, Hernandez MC, Bischofberger J.

Nat Commun. 2018 Sep 3;9(1):3576. doi: 10.1038/s41467-018-06004-8.

4.

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission.

Knoflach F, Hernandez MC, Bertrand D.

J Vis Exp. 2018 Aug 16;(138). doi: 10.3791/57842.

5.

Identification of a Corticohabenular Circuit Regulating Socially Directed Behavior.

Benekareddy M, Stachniak TJ, Bruns A, Knoflach F, von Kienlin M, Künnecke B, Ghosh A.

Biol Psychiatry. 2018 Apr 1;83(7):607-617. doi: 10.1016/j.biopsych.2017.10.032. Epub 2017 Dec 2.

PMID:
29336819
6.

mTORC1 Inhibition Corrects Neurodevelopmental and Synaptic Alterations in a Human Stem Cell Model of Tuberous Sclerosis.

Costa V, Aigner S, Vukcevic M, Sauter E, Behr K, Ebeling M, Dunkley T, Friedlein A, Zoffmann S, Meyer CA, Knoflach F, Lugert S, Patsch C, Fjeldskaar F, Chicha-Gaudimier L, Kiialainen A, Piraino P, Bedoucha M, Graf M, Jessberger S, Ghosh A, Bischofberger J, Jagasia R.

Cell Rep. 2016 Apr 5;15(1):86-95. doi: 10.1016/j.celrep.2016.02.090. Epub 2016 Mar 24.

7.

GABAA receptor-mediated neurotransmission: Not so simple after all.

Knoflach F, Hernandez MC, Bertrand D.

Biochem Pharmacol. 2016 Sep 1;115:10-7. doi: 10.1016/j.bcp.2016.03.014. Epub 2016 Mar 19.

PMID:
27002180
8.

Chemical conversion of human fibroblasts into functional Schwann cells.

Thoma EC, Merkl C, Heckel T, Haab R, Knoflach F, Nowaczyk C, Flint N, Jagasia R, Jensen Zoffmann S, Truong HH, Petitjean P, Jessberger S, Graf M, Iacone R.

Stem Cell Reports. 2014 Oct 14;3(4):539-47. doi: 10.1016/j.stemcr.2014.07.014. Epub 2014 Sep 11.

9.

Mapping the binding pocket of a novel, high-affinity, slow dissociating tachykinin NK3 receptor antagonist: biochemical and electrophysiological characterization.

Malherbe P, Knoflach F, Marcuz A, Bohnert C, Weber M, Knust H, Ratni H, Spooren W, Ballard TM, Bissantz C.

Neuropharmacology. 2014 Nov;86:259-72. doi: 10.1016/j.neuropharm.2014.07.017. Epub 2014 Aug 5.

PMID:
25107588
10.

Characterization of RO5126946, a Novel α7 nicotinic acetylcholine receptor-positive allosteric modulator.

Sahdeo S, Wallace T, Hirakawa R, Knoflach F, Bertrand D, Maag H, Misner D, Tombaugh GC, Santarelli L, Brameld K, Milla ME, Button DC.

J Pharmacol Exp Ther. 2014 Aug;350(2):455-68. doi: 10.1124/jpet.113.210963. Epub 2014 Jun 10.

PMID:
24917542
11.

Effect of bitopertin, a glycine reuptake inhibitor, on negative symptoms of schizophrenia: a randomized, double-blind, proof-of-concept study.

Umbricht D, Alberati D, Martin-Facklam M, Borroni E, Youssef EA, Ostland M, Wallace TL, Knoflach F, Dorflinger E, Wettstein JG, Bausch A, Garibaldi G, Santarelli L.

JAMA Psychiatry. 2014 Jun;71(6):637-46. doi: 10.1001/jamapsychiatry.2014.163.

PMID:
24696094
12.

Reducing GABAA α5 receptor-mediated inhibition rescues functional and neuromorphological deficits in a mouse model of down syndrome.

Martínez-Cué C, Martínez P, Rueda N, Vidal R, García S, Vidal V, Corrales A, Montero JA, Pazos Á, Flórez J, Gasser R, Thomas AW, Honer M, Knoflach F, Trejo JL, Wettstein JG, Hernández MC.

J Neurosci. 2013 Feb 27;33(9):3953-66. doi: 10.1523/JNEUROSCI.1203-12.2013.

13.

Cognitive impairment in major depression and the mGlu2 receptor as a therapeutic target.

Goeldner C, Ballard TM, Knoflach F, Wichmann J, Gatti S, Umbricht D.

Neuropharmacology. 2013 Jan;64:337-46. doi: 10.1016/j.neuropharm.2012.08.001. Epub 2012 Aug 23. Review.

PMID:
22992331
14.

Selective degeneration of septal and hippocampal GABAergic neurons in a mouse model of amyloidosis and tauopathy.

Loreth D, Ozmen L, Revel FG, Knoflach F, Wetzel P, Frotscher M, Metzger F, Kretz O.

Neurobiol Dis. 2012 Jul;47(1):1-12. doi: 10.1016/j.nbd.2012.03.011. Epub 2012 Mar 9.

PMID:
22426397
15.

Potentiation of sensory responses in ventrobasal thalamus in vivo via selective modulation of mGlu1 receptors with a positive allosteric modulator.

Salt TE, Jones HE, Andolina IM, Copeland CS, Clements JT, Knoflach F, Sillito AM.

Neuropharmacology. 2012 Mar;62(4):1695-9. doi: 10.1016/j.neuropharm.2011.11.015. Epub 2011 Dec 7.

16.

Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia.

Alberati D, Moreau JL, Lengyel J, Hauser N, Mory R, Borroni E, Pinard E, Knoflach F, Schlotterbeck G, Hainzl D, Wettstein JG.

Neuropharmacology. 2012 Feb;62(2):1152-61. doi: 10.1016/j.neuropharm.2011.11.008. Epub 2011 Nov 27.

PMID:
22138164
17.

Gantenerumab: a novel human anti-Aβ antibody demonstrates sustained cerebral amyloid-β binding and elicits cell-mediated removal of human amyloid-β.

Bohrmann B, Baumann K, Benz J, Gerber F, Huber W, Knoflach F, Messer J, Oroszlan K, Rauchenberger R, Richter WF, Rothe C, Urban M, Bardroff M, Winter M, Nordstedt C, Loetscher H.

J Alzheimers Dis. 2012;28(1):49-69. doi: 10.3233/JAD-2011-110977.

PMID:
21955818
18.

Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes.

Rudolph U, Knoflach F.

Nat Rev Drug Discov. 2011 Jul 29;10(9):685-97. doi: 10.1038/nrd3502. Review.

19.

Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK₁ and NK₃ receptors.

Malherbe P, Knoflach F, Hernandez MC, Hoffmann T, Schnider P, Porter RH, Wettstein JG, Ballard TM, Spooren W, Steward L.

Br J Pharmacol. 2011 Feb;162(4):929-46. doi: 10.1111/j.1476-5381.2010.01096.x.

20.

Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.

Woltering TJ, Wichmann J, Goetschi E, Knoflach F, Ballard TM, Huwyler J, Gatti S.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6969-74. doi: 10.1016/j.bmcl.2010.09.125. Epub 2010 Oct 21.

PMID:
20971004
21.

Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.

Ratni H, Ballard TM, Bissantz C, Hoffmann T, Jablonski P, Knoflach F, Knust H, Malherbe P, Nettekoven M, Patiny-Adam A, Riemer C, Schmitt M, Spooren W.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6735-8. doi: 10.1016/j.bmcl.2010.08.138. Epub 2010 Sep 17.

PMID:
20850972
22.

Enhanced dentate gyrus synaptic plasticity but reduced neurogenesis in a mouse model of amyloidosis.

Poirier R, Veltman I, Pflimlin MC, Knoflach F, Metzger F.

Neurobiol Dis. 2010 Nov;40(2):386-93. doi: 10.1016/j.nbd.2010.06.014. Epub 2010 Jul 6.

PMID:
20615468
23.

In vitro pharmacological selectivity profile of oseltamivir prodrug (Tamiflu) and active metabolite.

Lindemann L, Jacobsen H, Schuhbauer D, Knoflach F, Gatti S, Wettstein JG, Loetscher H, Chu T, Ebeling M, Paulson JC, Prinssen E, Brockhaus M.

Eur J Pharmacol. 2010 Feb 25;628(1-3):6-10. doi: 10.1016/j.ejphar.2009.11.020. Epub 2009 Nov 14.

24.

The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.

Knust H, Achermann G, Ballard T, Buettelmann B, Gasser R, Fischer H, Hernandez MC, Knoflach F, Koblet A, Stadler H, Thomas AW, Trube G, Waldmeier P.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. doi: 10.1016/j.bmcl.2009.08.053. Epub 2009 Aug 15.

PMID:
19762240
25.

Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA alpha5 inverse agonists with potential for the treatment of cognitive dysfunction.

Buettelmann B, Ballard TM, Gasser R, Fischer H, Hernandez MC, Knoflach F, Knust H, Stadler H, Thomas AW, Trube G.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5958-61. doi: 10.1016/j.bmcl.2009.08.027. Epub 2009 Aug 11.

PMID:
19740657
26.

Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.

Achermann G, Ballard TM, Blasco F, Broutin PE, Büttelmann B, Fischer H, Graf M, Hernandez MC, Hilty P, Knoflach F, Koblet A, Knust H, Kurt A, Martin JR, Masciadri R, Porter RH, Stadler H, Thomas AW, Trube G, Wichmann J.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5746-52. doi: 10.1016/j.bmcl.2009.07.153. Epub 2009 Aug 4.

PMID:
19726184
27.

Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.

Malherbe P, Borroni E, Pinard E, Wettstein JG, Knoflach F.

Mol Pharmacol. 2009 Sep;76(3):618-31. doi: 10.1124/mol.109.055152. Epub 2009 Jun 19.

PMID:
19542319
28.

Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers.

Vieira E, Huwyler J, Jolidon S, Knoflach F, Mutel V, Wichmann J.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9. doi: 10.1016/j.bmcl.2009.01.108. Epub 2009 Feb 6.

PMID:
19233648
29.

RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors.

Ballard TM, Knoflach F, Prinssen E, Borroni E, Vivian JA, Basile J, Gasser R, Moreau JL, Wettstein JG, Buettelmann B, Knust H, Thomas AW, Trube G, Hernandez MC.

Psychopharmacology (Berl). 2009 Jan;202(1-3):207-23. doi: 10.1007/s00213-008-1357-7. Epub 2008 Oct 21.

PMID:
18936916
30.

Characterization of behavioral response to amphetamine, tyrosine hydroxylase levels, and dopamine receptor levels in neurokinin 3 receptor knockout mice.

Nordquist RE, Savignac H, Pauly-Evers M, Walker G, Knoflach F, Borroni E, Glaentzlin P, Bohrmann B, Messer J, Ozmen L, Albientz A, Spooren W.

Behav Pharmacol. 2008 Sep;19(5-6):518-29. doi: 10.1097/FBP.0b013e32830cd7f5.

PMID:
18690106
31.

Characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptors.

Malherbe P, Masciadri R, Norcross RD, Knoflach F, Kratzeisen C, Zenner MT, Kolb Y, Marcuz A, Huwyler J, Nakagawa T, Porter RH, Thomas AW, Wettstein JG, Sleight AJ, Spooren W, Prinssen EP.

Br J Pharmacol. 2008 Jun;154(4):797-811. doi: 10.1038/bjp.2008.135. Epub 2008 Apr 21.

32.

Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.

Woltering TJ, Wichmann J, Goetschi E, Adam G, Kew JN, Knoflach F, Ballard TM, Huwyler J, Mutel V, Gatti S.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2725-9. doi: 10.1016/j.bmcl.2008.02.076. Epub 2008 Mar 5.

PMID:
18374569
33.

Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: part 2. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.

Woltering TJ, Adam G, Wichmann J, Goetschi E, Kew JN, Knoflach F, Mutel V, Gatti S.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1091-5. Epub 2007 Dec 8.

PMID:
18096387
34.

Asymmetric synthesis and receptor pharmacology of the group II mGlu receptor ligand (1S,2R,3R,5R,6S)-2-amino-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid-HYDIA.

Woltering TJ, Adam G, Huguenin P, Wichmann J, Kolczewski S, Gatti S, Bourson A, Kew JN, Richards G, Kemp JA, Mutel V, Knoflach F.

ChemMedChem. 2008 Feb;3(2):323-35.

PMID:
18058780
35.

Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1.

Woltering TJ, Adam G, Alanine A, Wichmann J, Knoflach F, Mutel V, Gatti S.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6811-5. Epub 2007 Oct 17.

PMID:
17964783
36.

9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers.

Vieira E, Huwyler J, Jolidon S, Knoflach F, Mutel V, Wichmann J.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4628-31.

PMID:
16099654
37.

Alkyl diphenylacetyl, 9H-xanthene- and 9H-thioxanthene-carbonyl carbamates as positive allosteric modulators of mGlu1 receptors.

Wichmann J, Bleicher K, Vieira E, Woltering T, Knoflach F, Mutel V.

Farmaco. 2002 Dec;57(12):989-92.

PMID:
12564473
38.

Identification and characterization of a novel splice variant of the metabotropic glutamate receptor 5 gene in human hippocampus and cerebellum.

Malherbe P, Kew JN, Richards JG, Knoflach F, Kratzeisen C, Zenner MT, Faull RL, Kemp JA, Mutel V.

Brain Res Mol Brain Res. 2002 Dec 30;109(1-2):168-78.

PMID:
12531526
39.

Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor.

Malherbe P, Kratochwil N, Knoflach F, Zenner MT, Kew JN, Kratzeisen C, Maerki HP, Adam G, Mutel V.

J Biol Chem. 2003 Mar 7;278(10):8340-7. Epub 2002 Dec 30.

40.

Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor.

Malherbe P, Knoflach F, Broger C, Ohresser S, Kratzeisen C, Adam G, Stadler H, Kemp JA, Mutel V.

Mol Pharmacol. 2001 Nov;60(5):944-54.

PMID:
11641422
41.

Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site.

Knoflach F, Mutel V, Jolidon S, Kew JN, Malherbe P, Vieira E, Wichmann J, Kemp JA.

Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7. Epub 2001 Oct 23. Erratum in: Proc Natl Acad Sci U S A 2001 Dec 18;98(26):15393.

42.

Pharmacological properties of native metabotropic glutamate receptors in freshly dissociated Golgi cells of the rat cerebellum.

Knoflach F, Woltering T, Adam G, Mutel V, Kemp JA.

Neuropharmacology. 2001;40(2):163-9.

PMID:
11114394
43.

Effect of metabotropic glutamate receptor activation on receptor-mediated cyclic AMP responses in primary cultures of rat striatal neurones.

Cartmell J, Goepfert F, Knoflach F, Pink JR, Bleuel Z, Richards JG, Schaffhauser H, Kemp JA, Wichmann J, Mutel V.

Brain Res. 1998 Apr 27;791(1-2):191-9.

PMID:
9593890
45.

Multiple pathways for regulation of the KCl-induced [3H]-GABA release by metabotropic glutamate receptors, in primary rat cortical cultures.

Schaffhauser H, Knoflach F, Pink JR, Bleuel Z, Cartmell J, Goepfert F, Kemp JA, Richards JG, Adam G, Mutel V.

Brain Res. 1998 Jan 26;782(1-2):91-104.

PMID:
9519253
46.

Pharmacological modulation of the diazepam-insensitive recombinant gamma-aminobutyric acidA receptors alpha 4 beta 2 gamma 2 and alpha 6 beta 2 gamma 2.

Knoflach F, Benke D, Wang Y, Scheurer L, Lüddens H, Hamilton BJ, Carter DB, Mohler H, Benson JA.

Mol Pharmacol. 1996 Nov;50(5):1253-61.

PMID:
8913357
47.

Modulation of voltage-gated calcium channels by orphanin FQ in freshly dissociated hippocampal neurons.

Knoflach F, Reinscheid RK, Civelli O, Kemp JA.

J Neurosci. 1996 Nov 1;16(21):6657-64.

48.

Benzodiazepine-insensitive mice generated by targeted disruption of the gamma 2 subunit gene of gamma-aminobutyric acid type A receptors.

Günther U, Benson J, Benke D, Fritschy JM, Reyes G, Knoflach F, Crestani F, Aguzzi A, Arigoni M, Lang Y, Bluethmann H, Mohler H, Lüscher B.

Proc Natl Acad Sci U S A. 1995 Aug 15;92(17):7749-53.

49.

Heterogeneity of GABAA-receptors: cell-specific expression, pharmacology, and regulation.

Mohler H, Knoflach F, Paysan J, Motejlek K, Benke D, Lüscher B, Fritschy JM.

Neurochem Res. 1995 May;20(5):631-6. Review.

PMID:
7643969
50.

Full and partial agonism displayed by benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes.

Knoflach F, Drescher U, Scheurer L, Malherbe P, Mohler H.

J Pharmacol Exp Ther. 1993 Jul;266(1):385-91.

PMID:
8392559

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