scholarly journals Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABAB receptors

2007 ◽  
Vol 17 (22) ◽  
pp. 6206-6211 ◽  
Author(s):  
Sébastien Guery ◽  
Philipp Floersheim ◽  
Klemens Kaupmann ◽  
Wolfgang Froestl
Keyword(s):  
Gabab Receptors ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators

Synthesis and Biological Activity of Allosteric Modulators of GABAB Receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines

2006 ◽  
Vol 59 (7) ◽  
pp. 445 ◽  
Author(s):  
David I. B. Kerr ◽  
Jennifer Ong ◽  
Michael V. Perkins ◽  
Rolf H. Prager ◽  
Ni Made Puspawati
Keyword(s):  
Biological Activity ◽  
Gabab Receptors ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators ◽  
Derivatives Of

A series of 15 analogues of fendiline, and 34 derivatives of N-(3-phenylpropyl)-1-arylethylamine have been prepared for evaluation as positive allosteric modulators of GABAB receptors. The most active (EC50, 10 nM) was N-(3,3-diphenylpropyl)-1-(3-chloro-4-methoxyphenyl)ethylamine 6g.

GABAB receptors as a therapeutic strategy in substance use disorders: Focus on positive allosteric modulators

2015 ◽  
Vol 88 ◽  
pp. 36-47 ◽  
Author(s):  
Małgorzata Filip ◽  
Małgorzata Frankowska ◽  
Anna Sadakierska-Chudy ◽  
Agata Suder ◽  
Łukasz Szumiec ◽  
...  
Keyword(s):  
Substance Use ◽  
Substance Use Disorders ◽  
Therapeutic Strategy ◽  
Gabab Receptors ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators
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