1055233-65-2Relevant academic research and scientific papers
Positron emission tomography to elucidate pharmacokinetic differences of regioisomeric retinoid x receptor agonists
Kobayashi, Toshiki,Furusawa, Yuki,Yamada, Shoya,Akehi, Masaru,Takenaka, Fumiaki,Sasaki, Takanori,Akahoshi, Akiya,Hanada, Takahisa,Matsuura, Eiji,Hirano, Hiroyuki,Tai, Akihiro,Kakuta, Hiroki
, p. 334 - 338 (2015)
RXR partial agonist NEt-4IB (2a, 6-[ethyl-(4-isobutoxy-3-isopropylphenyl)amino]pyridine-3-carboxylic acid: EC50 = 169 nM, Emax = 55%) showed a blood concentration higher than its Emax after single oral administration at 30 mg/kg to mice, and repeated oral administration at 10 mg/kg/day to KK-Ay mice afforded antitype 2 diabetes activity without the side effects caused by RXR full agonists. However, RXR full agonist NEt-3IB (1a), in which the isobutoxy and isopropyl groups of 2a are interchanged, gave a much lower blood concentration than 2a. Here we used positron emission tomography (PET) with tracers [11C]1a, [11C]2a and fluorinated derivatives [18F]1b, [18F]2b, which have longer half-lives, to examine the reason why 1a and 2a exhibited significantly different blood concentrations. As a result, the reason for the high blood concentration of 2a after oral administration was found to be linked to higher intestinal absorbability together with lower biliary excretion, compared with 1a.
Modification at the lipophilic domain of RXR agonists differentially influences activation of RXR heterodimers
Ohsawa, Fuminori,Morishita, Ken-Ichi,Yamada, Shoya,Makishima, Makoto,Kakuta, Hiroki
scheme or table, p. 521 - 525 (2011/03/19)
RXR permissive heterodimers are reported to be activated differently depending upon the chemical structure of RXR agonists, but the relationship of agonist structure to differential heterodimer activation has not been explored in detail. In this study, we
REXINOID COMPOUND HAVING ALKOXY GROUP
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, (2009/12/05)
Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R1 is selected from the group c
