- New class of bioluminogenic probe based on bioluminescent enzyme-induced electron transfer: BioLeT
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Bioluminescence imaging (BLI) has advantages for investigating biological phenomena in deep tissues of living animals, but few design strategies are available for functional bioluminescent substrates. We propose a new design strategy (designated as bioluminescent enzyme-induced electron transfer: BioLeT) for luciferin-based bioluminescence probes. Luminescence measurements of a series of aminoluciferin derivatives confirmed that bioluminescence can be controlled by means of BioLeT. Based on this concept, we developed bioluminescence probes for nitric oxide that enabled quantitative and sensitive detection even in vivo. Our design strategy should be applicable to develop a wide range of practically useful bioluminogenic probes.
- Takakura, Hideo,Kojima, Ryosuke,Kamiya, Mako,Kobayashi, Eiji,Komatsu, Toru,Ueno, Tasuku,Terai, Takuya,Hanaoka, Kenjiro,Nagano, Tetsuo,Urano, Yasuteru
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supporting information
p. 4010 - 4013
(2015/04/14)
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- Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5- benzodiazepin-2-ones; Potential imaging agents of the metabotropic glutamate 2 receptor
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A focused library of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones containing sites for 11C-, 18F- and 123I- labelling have been prepared and evaluated against membrane expressing human recombinant metabotropic glutamate 2 receptor (mGluR2). The compounds were found to be non-competitive antagonists with nanomolar affinity. HPLC evaluation of the physiochemical properties of these compounds identified two candidates for PET and SPECT imaging of mGluR2.
- Gilfillan, Lynne,Blair, Adele,Morris, Brian J.,Pratt, Judith A.,Schweiger, Lutz,Pimlott, Sally,Sutherland, Andrew
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p. 1118 - 1123
(2013/07/26)
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- NOVEL BENZODIAZEPINONES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR FUNCTIONS AND NEUROLOGICAL USES THEREOF
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The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also
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Paragraph 0124; 0125; 0128
(2013/03/28)
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- Glutamate receptor antagonists
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The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2and R3are as defined in the specification.
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- Glutamate receptor antagonists
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The present invention relates to compounds of with a base structure of formula 1 The compounds of formula I are shown to have activity as metabotropic glutamate receptor antagonists.
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