372523-75-6Relevant academic research and scientific papers
N-Acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist
Hirose, Masaaki,Egashira, Shin-Ichiro,Goto, Yasuhiro,Hashihayata, Takashi,Ohtake, Norikazu,Iwaasa, Hisashi,Hata, Mikiko,Fukami, Takehiro,Kanatani, Akio,Yamada, Koji
, p. 4497 - 4499 (2003)
The identification of potent and selective orexin-2 receptor (OX 2R) antagonists is described based on the modification of N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline analogue 1, recently discovered during high throughput screening (HTS). Substitution of an acyl group in 1 with tert-Leucine (tert-Leu), and introduction of a 4-pyridylmethyl substituent onto the amino function of tert-Leu improved compound potency, selectivity, and water solubility. Thus, compound 29 is a promising tool to investigate the role of orexin-2 receptors.
