357925-37-2Relevant academic research and scientific papers
Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists
Sato, Nagaaki,Jitsuoka, Makoto,Ishikawa, Shiho,Nagai, Keita,Tsuge, Hiroyasu,Ando, Makoto,Okamoto, Osamu,Iwaasa, Hisashi,Gomori, Akira,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro
scheme or table, p. 1670 - 1674 (2009/11/30)
Novel imidazoline derivatives were discovered to be potent neuropeptide Y Y5 receptor antagonists. High-throughput screening of Merck sample collections against the human Y5 receptor resulted in the identification of 2,4,4-triphenylimidazoline (1), which had an IC50 of 54 nM. Subsequent optimization led to the identification of several potent derivatives.
