852608-86-7Relevant articles and documents
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective α2C-adrenergic receptor antagonists
Hagihara, Koji,Kashima, Hajime,Iida, Kyoichiro,Enokizono, Junichi,Uchida, Shin-ichi,Nonaka, Hiromi,Kurokawa, Masako,Shimada, Junichi
, p. 1616 - 1621 (2007/10/03)
The synthesis of a series of 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methyl-2-arylbenzofuran and 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran-2-carboxamide derivatives as novel α2C-adrenergic receptor antagonists are described. Their affinity at three different human α2-adrenergic receptors is reported, and some of these compounds exhibited high affinity for the α2C-adrenergic receptor with high subtype selectivity. Among them, compound 10e has been found to show the anti-l-dopa-induced dyskinetic activity in marmosets. The structure-activity relationship of these compounds is also discussed.