Novel Styrylpyridines as Probes for SPECT Imaging of Amyloid Plaques
Department of Radiology and Pharmacology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA. Journal of Medicinal Chemistry
(Impact Factor: 5.45).
06/2007; 50(9):2157-65. DOI: 10.1021/jm070025+
We report a series of radioiodinated styrylpyridines as single photon emission computed tomography probes for imaging Abeta plaques in the brain of patients with Alzheimer's disease (AD). In vitro binding showed that all of the styrylpyridines displayed very good binding affinities in postmortem AD brain homogenates (Ki = 3.6 to 15.5 nM). No-carrier-added samples of 13a, 13b, 16a, 16b, and 16e (radioiodinated with 125I) were successfully prepared. The in vivo biodistribution in normal mice, at 2 min after injection, showed excellent initial brain penetrations (4.03, 6.22, 5.43, and 8.04% dose/g for [125I]13a, 13b, 16a, and 16b, respectively). Furthermore, in vitro autoradiography of AD brain sections showed that the high binding signal was specifically due to the presence of Abeta plaques. Taken together, these results strongly suggest that these styrylpyridines are useful for imaging Abeta plaques in the living human brain.
Available from: PubMed Central
- "Many radioiodinated imaging agents derived from Congo Red or thioflavin-T have been developed. Compounds 1 , 2 , 3 , 4 , 5 , and 6  (Figure 3) are thought to be derived from Congo Red. Although 1, 2, and 3 showed unfavorable pharmacokinetics in vivo such as low uptake into the brain and a slow washout, the radioactivity pharmacokinetics of 5 and 6 was much improved. "
[Show abstract] [Hide abstract]
ABSTRACT: The development of radiotracers for use in vivo to image β-amyloid (Aβ) plaques in cases of Alzheimer's disease (AD) is an important, active area of research. The presence of Aβ aggregates in the brain is generally accepted as a hallmark of AD. Since the only definitive diagnosis of AD is by postmortem staining of affected brain tissue, the development of techniques which enable one to image Aβ plaques in vivo has been strongly desired. Furthermore, the quantitative evaluation of Aβ plaques in the brain could facilitate evaluation of the efficacy of antiamyloid therapies currently under development. This paper reviews the current situation in the development of agents for SPECT-based imaging of Aβ plaques in Alzheimer's brains.
04/2011; 2011:543267. DOI:10.1155/2011/543267
[Show abstract] [Hide abstract]
ABSTRACT: This paper describes a new approach to the evaluation of loss
adjustment factors for distribution systems. Such factors are required
for `use of system' and wheeling calculations and reflect the amount by
which purchases of energy at entry points to the system must exceed
consumption at the point of use to account for the losses which occur in
between. Renewed interest in cost-reflective methods of charging for
losses has resulted from the deregulation of the electricity supply
industry in many parts of the world. An algorithm is described which
combines the use of graph theory with readily available load flow
results, to assign the losses in each line or transformer within the
system to the consumers supplied by it. The resulting allocation is
shown to account for the voltage level, location and consumption pattern
of the consumer in a way which is economically efficient. A variety of
strategies for apportioning losses between multiple consumers at a given
location can be implemented. The algorithm is suitable for allocating
both demand and energy losses. Results on a full size distribution
network are presented, and are compared with traditional published loss
Power Industry Computer Application Conference, 1995. Conference Proceedings., 1995 IEEE; 06/1995
Available from: viamedica.pl
Nuclear medicine review. Central & Eastern Europe: journal of Bulgarian, Czech, Macedonian, Polish, Romanian, Russian, Slovak, Yugoslav societies of nuclear medicine and Ukrainian Society of Radiology 02/2007; 10(2):116-24.
Data provided are for informational purposes only. Although carefully collected, accuracy cannot be guaranteed. The impact factor represents a rough estimation of the journal's impact factor and does not reflect the actual current impact factor. Publisher conditions are provided by RoMEO. Differing provisions from the publisher's actual policy or licence agreement may be applicable.