56416-46-7Relevant academic research and scientific papers
THIENO-PYRIDINE DERIVATIVES AS GABA-B ALLOSTERIC ENHANCERS
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Page/Page column 26; 27, (2008/06/13)
The present invention relates to compounds of formula (I), Wherein R1 to R5 are as defined in the specification which compounds are active on the GABABreceptor and can be used for the manufacture of medicaments useful for treating CNS disorders.
Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor
Baraldi, Pier Giovanni,Zaid, Abdel Naser,Lampronti, Ilaria,Fruttarolo, Francesca,Pavani, Maria Giovanna,Tabrizi, Mojgan Aghazadhe,Shryock, John C.,Leung, Edward,Romagnoli, Romeo
, p. 1953 - 1957 (2007/10/03)
New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 μM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor. Compounds 4e and 4o appeared to be allosteric enhancers at a low concentration and antagonists at a higher concentration, whereas compounds 3c, 3g, 3s and 4l appeared to be weak antagonists that are also allosteric enhancers at the higher concentration of 10 μM. (C) 2000 Elsevier Science Ltd.
