188863-55-0Relevant academic research and scientific papers
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists
Conway, Richard J.,Valant, Celine,Christopoulos, Arthur,Robertson, Alan D.,Capuano, Ben,Crosby, Ian T.
supporting information; experimental part, p. 2560 - 2564 (2012/05/05)
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.
New μ-opioid receptor agonists with phenoxyacetic acid moiety
Sato, Susumu,Komoto, Teruo,Kanamaru, Yoshihiko,Kawamoto, Noriyuki,Okada, Tomomi,Kaiho, Terumitsu,Mogi, Kinichi,Morimoto, Shinichi,Umehara, Norimitsu,Koda, Tadayuki,Miyashita, Akira,Sakamoto, Takao,Niino, Yasuhiro,Oka, Tetsuo
, p. 292 - 297 (2007/10/03)
New μ-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, [2-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4-yl] phenoxy]acetic acid (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of δ- and κ-opioid receptors (DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat.
New strong fibrates with piperidine moiety
Komoto, Teruo,Hirota, Hiroyuki,Otsuka, Mari,Kotake, Jiro,Hasegawa, Susumu,Koya, Hidehiko,Sato, Susumu,Sakamoto, Takao
, p. 1978 - 1985 (2007/10/03)
New fibrates containing piperidine, 4-hydroxypiperidine, piperidin-3-ene, and piperazine moieties in the structures were synthesized and evaluated. Among the synthesized compounds, 2-[3-[1-(4-fluorobenzoyl)-piperidin-4yl]phenoxy]-2-methylpropanoic acid (9
