Synthesis and Pharmacological Characterization of 2-(Acylamino)thiophene Derivatives as Metabolically Stable, Orally Effective, Positive Allosteric Modulators of the GABABReceptor

Claudia Mugnaini; Valentina Pedani; Angelo Casu; Carla Lobina; Alberto Casti; Paola Maccioni; Alessandra Porcu; Daniela Giunta; Stefania Lamponi; Maurizio Solinas; Stefania Dragoni; Massimo Valoti; Giancarlo Colombo; Maria Paola Castelli; Gian Luigi Gessa; Federico Corelli

doi:10.1021/jm400144w

Synthesis and Pharmacological Characterization of 2-(Acylamino)thiophene Derivatives as Metabolically Stable, Orally Effective, Positive Allosteric Modulators of the GABABReceptor

Journal of Medicinal Chemistry ◽

10.1021/jm400144w ◽

2013 ◽

Vol 56 (9) ◽

pp. 3620-3635 ◽

Cited By ~ 25

Author(s):

Claudia Mugnaini ◽

Valentina Pedani ◽

Angelo Casu ◽

Carla Lobina ◽

Alberto Casti ◽

...

Keyword(s):

Allosteric Modulators ◽

Pharmacological Characterization ◽

Thiophene Derivatives ◽

Positive Allosteric Modulators

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Pharmacological Characterization of Natural Tobacco Alkaloids in the Presence of Positive Allosteric Modulators Against Human α4β2 and α7 Nicotinic Acetylcholine Receptors

Biophysical Journal ◽

10.1016/j.bpj.2019.11.790 ◽

2020 ◽

Vol 118 (3) ◽

pp. 119a

Author(s):

Omar Alijevic ◽

Damian Mc Hugh ◽

Anatoly Mazurov ◽

Julia Hoeng ◽

Manuel Peitsch

Keyword(s):

Nicotinic Acetylcholine Receptors ◽

Acetylcholine Receptors ◽

Allosteric Modulators ◽

Pharmacological Characterization ◽

Nicotinic Acetylcholine ◽

Α7 Nicotinic Acetylcholine Receptors ◽

Tobacco Alkaloids ◽

Positive Allosteric Modulators

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Pharmacological Characterization of cGMP Regulation by the Biarylpropylsulfonamide Class of Positive, Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptors

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.106.105734 ◽

2006 ◽

Vol 319 (1) ◽

pp. 293-298 ◽

Cited By ~ 11

Author(s):

John W. Ryder ◽

Julie F. Falcone ◽

Jason R. Manro ◽

Kjell A. Svensson ◽

Kalpana M. Merchant

Keyword(s):

Allosteric Modulators ◽

Pharmacological Characterization ◽

Positive Allosteric Modulators

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Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces

Journal of Chemical Information and Modeling ◽

10.1021/ci500559b ◽

2014 ◽

Vol 54 (12) ◽

pp. 3404-3416 ◽

Cited By ~ 14

Author(s):

Ann-Beth Nørholm ◽

Pierre Francotte ◽

Eric Goffin ◽

Iuliana Botez ◽

Laurence Danober ◽

...

Keyword(s):

Ligand Binding ◽

Glutamate Receptor ◽

Computational Methods ◽

Driving Forces ◽

Binding Domain ◽

Ligand Binding Domain ◽

Allosteric Modulators ◽

Thermodynamic Characterization ◽

Positive Allosteric Modulators

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Characterization of the effects of novel positive allosteric modulators on the functionality of the α7 nicotinic acetylcholine receptor (nAChR)

The FASEB Journal ◽

10.1096/fasebj.2018.32.1_supplement.533.80 ◽

2018 ◽

Vol 32 (S1) ◽

Author(s):

Francis Reilly‐Andujar ◽

José A. Lasalde ◽

José O. Colón

Keyword(s):

Acetylcholine Receptor ◽

Nicotinic Acetylcholine Receptor ◽

Allosteric Modulators ◽

Α7 Nicotinic Acetylcholine Receptor ◽

Nicotinic Acetylcholine ◽

Positive Allosteric Modulators

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Reprint of Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2

Neuropharmacology ◽

10.1016/j.neuropharm.2016.08.040 ◽

2017 ◽

Vol 115 ◽

pp. 115-127 ◽

Cited By ~ 5

Author(s):

L. Lundström ◽

C. Bissantz ◽

J. Beck ◽

M. Dellenbach ◽

T.J. Woltering ◽

...

Keyword(s):

Molecular Characterization ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT2C Receptor

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b00401 ◽

2018 ◽

Vol 62 (1) ◽

pp. 288-305 ◽

Cited By ~ 11

Author(s):

Christopher T. Wild ◽

Joanna M. Miszkiel ◽

Eric A. Wold ◽

Claudia A. Soto ◽

Chunyong Ding ◽

...

Keyword(s):

Synthesis And Characterization ◽

Allosteric Modulators ◽

Design Synthesis ◽

Positive Allosteric Modulators

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Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2

Neuropharmacology ◽

10.1016/j.neuropharm.2016.08.032 ◽

2016 ◽

Vol 111 ◽

pp. 253-265 ◽

Cited By ~ 3

Author(s):

L. Lundström ◽

C. Bissantz ◽

J. Beck ◽

M. Dellenbach ◽

T.J. Woltering ◽

...

Keyword(s):

Molecular Characterization ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Synthesis and pharmacological characterization of new silicon-based W84-type allosteric modulators for ligand binding to muscarinic M2 receptors

Journal of Organometallic Chemistry ◽

10.1016/s0022-328x(03)00553-9 ◽

2003 ◽

Vol 686 (1-2) ◽

pp. 75-83 ◽

Cited By ~ 6

Author(s):

Seraina Duda-Johner ◽

Jürgen O Daiß ◽

Klaus Mohr ◽

Reinhold Tacke

Keyword(s):

Ligand Binding ◽

Allosteric Modulators ◽

Pharmacological Characterization ◽

Silicon Based ◽

Muscarinic M2 Receptors

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Characterization of novel selective positive allosteric modulators (PAMS) of the M4 muscarinic acetylcholine receptor (mAChR)

The FASEB Journal ◽

10.1096/fasebj.22.1_supplement.714.2 ◽

2008 ◽

Vol 22 (S1) ◽

Author(s):

Ashley Elizabeth Brady ◽

Tom M Bridges ◽

Carrie K Jones ◽

Jana K Shirey ◽

Craig W Lindsley ◽

...

Keyword(s):

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Allosteric Modulators ◽

Muscarinic Acetylcholine ◽

Positive Allosteric Modulators

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Characterization of COR627 and COR628, Two Novel Positive Allosteric Modulators of the GABAB Receptor

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.111.186460 ◽

2011 ◽

Vol 340 (3) ◽

pp. 529-538 ◽

Cited By ~ 34

Author(s):

M. Paola Castelli ◽

Angelo Casu ◽

Paola Casti ◽

Carla Lobina ◽

Mauro A. M. Carai ◽

...

Keyword(s):

Gabab Receptor ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

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