- Electric-field-responsive handle for large-area orientation of discotic liquid-crystalline molecules in millimeter-thick films
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Current events: An electric-field-responsive handle (see picture) was developed that enables large-area and millimeter-thick unidirectional orientation of columnarly assembled π-conjugated liquid-crystalline molecules. The handles in the columns are hydrogen-bonded and align along the direction of an applied electric field.
- Miyajima, Daigo,Araoka, Fumito,Takezoe, Hideo,Kim, Jungeun,Kato, Kenichi,Takata, Masaki,Aida, Takuzo
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p. 7865 - 7869
(2011/10/08)
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- Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain
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Fatty acid amide hydrolyase (FAAH) is one of the main enzymes responsible for terminating the signaling of endocannabinoids in the brain. Imaging FAAH in vivo using PET or SPECT is important to deeper understanding of its role in neuropsychiatric disorders. However, at present, no radioligand is available for mapping the enzyme in vivo. Here, we synthesized 18 aryl analogues of anandamide, FAAH's endogenous substrate, and in vitro evaluated their potential as metabolic trapping tracers. Interaction studies with recombinant FAAH revealed good to very good interaction of the methoxy substituted aryl anandamide analogues 17, 18, 19, and 20 with FAAH and they were identified as competing substrates. Compounds 17 and 18 did not display significant binding to CB1 and CB2 cannabinoid receptors and stand out as potential candidate metabolic trapping tracers. They were successfully labeled with 11C in good yields and high radiochemical purity and displayed brain uptake in C57BL/6J mice. Radioligands [11C]-17 and [ 11C]-18 merit further investigation in vivo.
- Wyffels, Leonie,Muccioli, Giulio G.,De Bruyne, Sylvie,Moerman, Lieselotte,Sambre, Johan,Lambert, Didier M.,De Vos, Filip
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supporting information; experimental part
p. 4613 - 4622
(2010/02/28)
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- Aryl aniline beta2 adrenergic receptor agonists
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The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
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