Synthesis and Biological Evaluation of 2,3,5-Substituted [1,2,4]Thiadiazoles as Allosteric Modulators of Adenosine Receptors

2004 ◽  
Vol 47 (3) ◽  
pp. 663-672 ◽  
Author(s):  
Adrianus M. C. H. van den Nieuwendijk ◽  
Daniele Pietra ◽  
Laura Heitman ◽  
Anikó Göblyös ◽  
Adriaan P. IJzerman
Keyword(s):  
Adenosine Receptors ◽  
Biological Evaluation ◽  
Allosteric Modulators ◽  
Synthesis And Biological Evaluation

Fulgazepam: A Fulgimide-Based Potentiator of GABAA Receptors

2019 ◽  
Author(s):  
Karin Rustler ◽  
Galyna Maleeva ◽  
Alexandre M. J. Gomila ◽  
Pau Gorostiza ◽  
Piotr Bregestovski ◽  
...  
Keyword(s):  
Protein Function ◽  
Biological Evaluation ◽  
Term Treatment ◽  
Allosteric Modulators ◽  
Design Synthesis ◽  
Non Invasive ◽  
Long Term Treatment ◽  
Benzodiazepine Derivatives ◽  
Synthesis And Biological Evaluation

The <i>γ</i>-aminobutyric acid gated chloride channel represents the major mediator of inhibitory neurotransmission in the mammalian central nervous system and its dysfunction is related to severe diseases like epilepsy and depression, which can be relieved by the application of allosteric modulators. However, the drugs’ potential side-effects limit their application for long-term treatment. Applying light as external stimulus to modify the pharmacophore’s activity, as emerged in the field of photopharmacology, provides a non-invasive tool with high spatial and temporal resolution for the modulation of protein function. Herein, we report the design, synthesis, and biological evaluation of photochromic fulgimide-based benzodiazepine derivatives as light-controllable potentiators of GABA<sub>A</sub> receptors (GABA<sub>A</sub>Rs). A photocontrolled potentiator of GABA<sub>A</sub>Rs (Fulgazepam) has been identified that does not display agonist or antagonist activity and allows manipulating zebrafish larvae swimming.

scholarly journals Targeting the Kv11.1 (hERG) channel with allosteric modulators. Synthesis and biological evaluation of three novel series of LUF7346 derivatives

2020 ◽  
pp. 113033
Author(s):  
Jacobus P.D. van Veldhoven ◽  
Giulia Campostrini ◽  
Constantijn J.E. van Gessel ◽  
Dorien Ward-van Oostwaard ◽  
Rongfang Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Herg Channel ◽  
Allosteric Modulators ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel

2015 ◽  
Vol 106 ◽  
pp. 50-59 ◽  
Author(s):  
Zhiyi Yu ◽  
Jacobus P.D. van Veldhoven ◽  
Ingrid M.E. 't Hart ◽  
Adrian H. Kopf ◽  
Laura H. Heitman ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Herg Channel ◽  
Allosteric Modulators ◽  
Synthesis And Biological Evaluation

scholarly journals Fulgazepam: A Fulgimide-Based Potentiator of GABAA Receptors

2019 ◽  
Author(s):  
Karin Rustler ◽  
Galyna Maleeva ◽  
Alexandre M. J. Gomila ◽  
Pau Gorostiza ◽  
Piotr Bregestovski ◽  
...  
Keyword(s):  
Protein Function ◽  
Biological Evaluation ◽  
Term Treatment ◽  
Allosteric Modulators ◽  
Design Synthesis ◽  
Non Invasive ◽  
Long Term Treatment ◽  
Benzodiazepine Derivatives ◽  
Synthesis And Biological Evaluation

The <i>γ</i>-aminobutyric acid gated chloride channel represents the major mediator of inhibitory neurotransmission in the mammalian central nervous system and its dysfunction is related to severe diseases like epilepsy and depression, which can be relieved by the application of allosteric modulators. However, the drugs’ potential side-effects limit their application for long-term treatment. Applying light as external stimulus to modify the pharmacophore’s activity, as emerged in the field of photopharmacology, provides a non-invasive tool with high spatial and temporal resolution for the modulation of protein function. Herein, we report the design, synthesis, and biological evaluation of photochromic fulgimide-based benzodiazepine derivatives as light-controllable potentiators of GABA<sub>A</sub> receptors (GABA<sub>A</sub>Rs). A photocontrolled potentiator of GABA<sub>A</sub>Rs (Fulgazepam) has been identified that does not display agonist or antagonist activity and allows manipulating zebrafish larvae swimming.

A3 adenosine receptors: Synthesis and biological evaluation of new potent and selective ligands

2005 ◽  
Author(s):  
Rosaria Volpini ◽  
Catia Lambertucci ◽  
Sara Taffi ◽  
Sauro Vittori ◽  
Karl-Norbert Klotz ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
Biological Evaluation ◽  
Selective Ligands ◽  
Synthesis And Biological Evaluation
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