109558-14-7Relevant articles and documents
1-(2′-Bromobenzyl)-6,7-dihydroxy- N-methyl-tetrahydroisoquinoline and 1,2-Demethyl-nuciferine as Agonists in Human D2 Dopamine Receptors
Cabedo, Nuria,Cortes, Diego,Loza, Mabel,Marques, Patrice,Moreno, Laura,Silva, Andrea G.,Vila, Laura,Castro, Marián,Sanz, María-Jesús
, (2020)
Certain D2-like dopamine receptor (DR) agonists are useful therapeutically as antiparkinsonian drugs, whereas D2-like DR antagonists or partial agonists are proven effective as antipsychotics. Two isoquinoline derivatives, 1-(2′-brom
Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HT2 and α1 receptor antagonists
Heng, Hui Li,Chee, Chin Fei,Chin, Sek Peng,Ouyang, Yifan,Wang, Hao,Buckle, Michael J.C.,Herr, Deron R.,Paterson, Ian C.,Doughty, Stephen W.,Abd Rahman, Noorsaadah,Chung, Lip Yong
, p. 576 - 582 (2018)
In this study, the (S)-enantiomers of the aporphine alkaloids, nuciferine and roemerine, were prepared via a synthetic route involving catalytic asymmetric hydrogenation and both stereoisomers were evaluated in vitro for functional activity at human 5-HT2 and adrenergic α1 receptor subtypes using a transforming growth factor-α shedding assay. Both enantiomers of each of the compounds were found to act as antagonists at 5-HT2 and α1 receptors. (R)-roemerine was the most potent compound at 5-HT2A and 5-HT2C receptors (pKb = 7.8-7.9) with good selectivity compared to (S)-roemerine at these two receptors and compared to its activity at 5-HT2B, α1A, α1B and α1D receptors.
Synthesis of pyrido[2,1-a]isoquinolin-4-ones and oxazino[2,3-a]isoquinolin- 4-ones: New inhibitors of mitochondrial respiratory chain
Moreno, Laura,Cabedo, Nuria,Boulangé, Agathe,Párraga, Javier,Galán, Abraham,Leleu, Stéphane,Sanz, María-Jesús,Cortes, Diego,Franck, Xavier
, p. 69 - 76 (2013/10/01)
Benzo[a]quinolizine is an important heterocyclic framework that can be found in numerous bioactive compounds. The general scheme for the synthesis of these compounds was based on the preparation of the appropriate dihydroisoquinolines by Bischler-Napieral