- IMAGING AGENTS WITH IMPROVED PHARMACOKINETIC PROFILES
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The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.
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Page/Page column 19
(2010/02/15)
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- Synthesis and radioiodination of some 9-aminoacridine derivatives for potential use in radionuclide therapy
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Three derivatives of the DNA intercalating compound 9-aminoacridine, were prepared and radioiodinated for biological experiments. The compounds are the stannyl derivatives 3-{4-[3-(acridin-9-ylamino)-propoxy]-3-trimethylstannyl- phenyl}-propionic acid and acridin-9-yl-{3-[4-(2-amino-ethyl)-2- trimethylstannyl-phenoxy]-propyl}-amine which were synthesized from the corresponding iodo derivatives by palladium catalyzed reactions, and 4-[2-(acridin-9-ylamino)-ethyl]-phenol. The two stannylated compounds and the phenol were used as precursors for radioiodination and were labeled with 125I using chloramine-T as an oxidant achieving high-to-excellent yields. Copyright
- Ghirmai, Senait,Mume, Eskender,Lundqvist, Hans,Tolmachev, Vladimir,Sjoeberg, Stefan
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p. 855 - 871
(2007/10/03)
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- INHIBITOR IMAGING AGENTS
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The present invention discloses that imaging agents which comprise a specific type of matrix metalloproteinase inhibitors (MMPi's) of the sulphonamide hydroxamate class labelled with an imaging moiety, are useful diagnostic imaging agents for in vivo imag
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Page/Page column 44
(2010/02/12)
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- Near-Infrared Heavy-Atom-Modified Fluorescent Dyes for Base-Calling in DNA-Sequencing Applications Using Temporal Discrimination
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A series of near-IR fluorescent dyes were prepared which contained an intramolecular heavy atom for altering the fluorescence lifetimes to produce a set of probes appropriate for base-calling in a single-lane DNA sequencing format. The heavy-atom modifica
- Flanagan Jr., James H.,Owens, Clyde V.,Romero, Sarah E.,Waddell, Emanuel,Kahn, Shaheer H.,Hammer, Robert P.,Soper, Steven A.
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p. 2676 - 2684
(2007/10/03)
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- Determination of serum biotinidase activity with biotinyl derivatives of iodotyramines as substrates
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We synthesized biotinylated mono- and di-iodotyramine and their radioactive counterparts and used these substances as substrates to estimate serum biotinidase activity in a radioassay system. The K(m) values determined for mono- and di-iodobiotinyl derivatives were 15.8 and 25.9 μM, respectively, whereas, the maximum velocities of the enzymatic reaction were 27.0 and 8.7 nmol · min-1 · mL-1, respectively. Both substrates competed with biocytin for the same active site of the enzyme and the K(i) values were 7.30 and 9.56 μM for the mono- and di-iodinated substrate, respectively. Higher assay sensitivity was obtained using [125I]biotinyl- monoiodotyramine as substrate, and the values obtained were directly related with those determined with the well-established colorimetric method (r = 0.9377, n = 31). However, for routine use, the assay may be accomplished by diluting the radiotracer with biocytin instead of its 'cold' counterpart, because it is a commercially available reagent. The values obtained in this case were very well correlated with those determined by the colorimetric assay as well (r = 0.9289, n = 31).
- Evangelatos,Kakabakos,Evangelatos,Ithakissios
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p. 1228 - 1231
(2007/10/02)
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