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A Phenylbenzothiazole conjugate with the Tricarbonyl fac-M(I)(CO)(3)](+) (M=Re, Tc-99, Tc-99m) core for imaging of beta-amyloid plaques


Sagnou, Marina; Tzanopoulou, Stamatia; Raptopoulou, Catherine P; Psycharis, Vassilis; Braband, Henrik; Alberto, Roger; Pirmettis, Ioannis C; Papadopoulos, Minas; Pelecanou, Maria (2012). A Phenylbenzothiazole conjugate with the Tricarbonyl fac-M(I)(CO)(3)](+) (M=Re, Tc-99, Tc-99m) core for imaging of beta-amyloid plaques. European Journal of Inorganic Chemistry, 2012(27):4279-4286.

Abstract

The 2-(4'-aminophenyl)-6-methylbenzothiazole that is known to display affinity and specificity toward the amyloid plaques of Alzheimer's disease (AD) has been joined to the tricarbonyl M(CO)3NNO] chelate (M = Re, 99Tc, and 99mTc) through a five-carbon linker chain to generate the neutral complex 1 (namely, Re-1 for M = Re; 99Tc-1 for M = 99Tc; and 99mTc-1 for M = 99mTc) with the aim of developing a single-photon emission computed tomography (SPECT) radiodiagnostic agent for AD. Re-1 was characterized by spectroscopic methods and X-ray crystallography, whereas the detailed NMR spectroscopic analysis of 99Tc-1 demonstrated its structural similarity to Re-1. Complexes Re-1 and 99Tc-1 display selective binding affinity for amyloid plaques as evidenced by fluorescence spectroscopy, whereas the biodistribution data of 99mTc-1?characterized by relatively low brain uptake, fast clearance from brain and blood, and in vivo stability?are considered encouraging for further elaboration on the structural features of 1 in the direction of increased brain uptake.

Abstract

The 2-(4'-aminophenyl)-6-methylbenzothiazole that is known to display affinity and specificity toward the amyloid plaques of Alzheimer's disease (AD) has been joined to the tricarbonyl M(CO)3NNO] chelate (M = Re, 99Tc, and 99mTc) through a five-carbon linker chain to generate the neutral complex 1 (namely, Re-1 for M = Re; 99Tc-1 for M = 99Tc; and 99mTc-1 for M = 99mTc) with the aim of developing a single-photon emission computed tomography (SPECT) radiodiagnostic agent for AD. Re-1 was characterized by spectroscopic methods and X-ray crystallography, whereas the detailed NMR spectroscopic analysis of 99Tc-1 demonstrated its structural similarity to Re-1. Complexes Re-1 and 99Tc-1 display selective binding affinity for amyloid plaques as evidenced by fluorescence spectroscopy, whereas the biodistribution data of 99mTc-1?characterized by relatively low brain uptake, fast clearance from brain and blood, and in vivo stability?are considered encouraging for further elaboration on the structural features of 1 in the direction of increased brain uptake.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:2012
Deposited On:01 Mar 2013 10:19
Last Modified:07 Dec 2017 20:09
Publisher:Wiley-Blackwell
ISSN:1434-1948
Publisher DOI:https://doi.org/10.1002/ejic.201200450

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