50461-51-3Relevant academic research and scientific papers
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists
Kim, Eunkyung,Park, Chan Sun,Han, Taedong,Bae, Myung-Ho,Chong, Wonee,Lee, Choong Hyun,Shin, Young Ah,Ahn, Byung-Nak,Kim, Mi Kyung,Shin, Chang Yell,Son, Moon Ho,Kim, Jin Kwan,Moon, Ho Sang,Shim, Hyun Joo,Kim, Eun Jung,Kim, Soon Hoe,Lim, Joong In,Lee, Chun Ho
scheme or table, p. 4993 - 4996 (2009/05/26)
Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.
Adrenoceptor and Tetrabenazine Antagonism Activities of Some Pyridinyltetrahydropyridines
Saari, Walfred S.,Halczenko, Wasyl,Huff, Joel R.,Guare, James P.,Hunt, Cecilia A.,et al.
, p. 1182 - 1185 (2007/10/02)
A series of pyridinyltetrahydropyridine derivatives was synthesized and evaluated as adrenoceptor and tetrabenazine antagonists. 4-(3-Fluoro-2-pyridinyl)-1,2,5,6-tetrahydropyridine proved to be the most potent and selective α2-adrenoceptor antagonist of the series as measured in vitro by displacement of 3H>clonidine and 3H>prazosin from membrane binding sites of calf cerebral cortex and by antagonism of the effects of clonidine and methoxamine in the rat isolated, field-stimulated vas deferens.In addition, this compound, and the corresponding desfluoro derivative, blocked tetrabenazine-induced ptosis in the mouse.
