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Ln[DO3A-N-α-(pyrenebutanamido)propionate] complexes: optimized relaxivity and N...
Ferreira, M. F.; Pereira, G.; Martins, A. F.; Martins, C. I. O.; Prata, M. I. M.; Petoud, S.; Toth, E.; Ferreira, P. M. T.; Martins, J. A.We have proposed recently that the DO3A-N-α-(amino)propionate chelator and its amide conjugates are leads to targeted, high relaxivity, safe contrast agents for magnetic resonance imaging. In this work we illustrate further the expeditious nature and robustness of the synthetic methodologies developed by preparing the DO3A-N-(α-pyrenebutanamido)propionate chelator. Its Gd3+ chelate retains the optimized water e...
Studies on the biodistribution of dextrin nanoparticles
Gonçalves, Clarisse; Ferreira, M. F. M.; Santos, A. C.; Prata, M. I. M.; Martins, J. A.; Geraldes, Carlos F. G. C.; Gama, F. M.The characterization of biodistribution is a central requirement in the development of biomedical applications based on the use of nanoparticles, in particular for controlled drug delivery. The blood circulation time, organ biodistribution and rate of excretion must be well characterized in the process of product development. In this work, the biodistribution of recently developed self-assembled dextrin nanopar...
First in vivo MRI assessment of a self-assembled metallostar compound endowed w...
Livramento, J. B.; Weidensteiner, C.; Prata, M. I. M.; Allegrini, P. R.; Geraldes, C. F. G. C.; Helm, L.; Kneuer, R.; Merbach, A. E.; Santos, A. C.Fe[Gd2bpy(DTTA)2(H2O)4]34- is a self-assembled, metallostar-structured potential MRI contrast agent, with six efficiently relaxing Gd3+ centres confined into a small molecular space. Its proton relaxivity is particularly remarkable at very high magnetic fields (r1 = 15.8 mM-1 s-1 at 200 MHz, 37°C, in H2O). Here we report the first in vivo MRI feasibility study, complemented with dynamic gamma scintigraphic imag...
Targeting of lanthanide(III) chelates of DOTA-type glycoconjugates to the hepat...
Prata, M. I. M.; Santos, A. C.; Torres, S.; André, J. P.; Martins, J. A.; Neves, M.; García-Martín, M. L.; Rodrigues, T. B.; López-Larrubia, P.The characterization of a new class of hydrophilic liver-targeted agents for gamma-scintigraphy and MRI, consisting, respectively, of [153Sm]3+ or Gd3+ complexes of DOTA monoamide or bisamide linked glycoconjugates (DOTA = 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), is reported. In vitro studies show high uptake of radiolabeled [153Sm]-DOTAGal2 by the human hepatocyte carcinoma cell line Hep G2 c...
Targeting of lanthanide(III) chelates of DOTA-type glycoconjugates to the hepat...
Prata, M. I. M.; Santos, A. C.; Torres, Susana; André, João P.; Martins, J. A. R.; Neves, M.; García Martín, M. L.; Rodrigues, T. B.; López Larrubia, P.The characterization of a new class of hydrophilic liver-targeted agents for gamma-scintigraphy and MRI, consisting, respectively, of [153Sm]3+ or Gd3+ complexes of DOTA monoamide or bisamide linked glycoconjugates (DOTA = 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), is reported. In vitro studies show high uptake of radiolabeled 153SmDOTAGal2 by the human hepatocyte carcinoma cell line Hep G2 cont...
Lanthanide(III) complexes of DOTA-glycoconjugates : a potential new class of le...
André, João P.; Geraldes, Carlos F. G. C.; Martins, J. A. R.; Merbach, André E.; Prata, M. I. M.; Santos, A. C.; Lima, J. J. Pedroso de; Tóth, ÉvaThe synthesis and characterization of a new class of DOTA (1,4,7,10-tetrakis(carboxymethyl)-1,4,7,10-tetraazacyclododecane) monoamide-linked glycoconjugates (glucose, lactose and galactose) of different valencies (mono, di and tetra) and their Sm(III), Eu(III) and Gd(III) complexes are reported. The proton NMR spectrum of Eu(III)-DOTALac(III) shows the predominance of a single structural isomer of square ...
Macrocyclic and polymeric lanthanide chelates: from physico-chemical studies to...
Duarte, M. G.; Prata, M. I. M.; Gil, M. H. M.; Geraldes, C. F. G. C.The improvement of commonly used Gd3+-based MRI contrast agents requires the design of new chelates with optimised in vivo efficacy, pharmacokinetic properties and specificity. The molecular parameters determining the nuclear relaxivity of the cationic chelate [Gd(DO2A)]+, as well as of some copolymers of [Gd(DTPA)]2- with diamines, were obtained using spectroscopic techniques. In both cases, the resulting too ...
153Sm3+ and 111In3+ DTPA derivatives with high hepatic specificity: in vivo and...
Prata, M. I. M.; Santos, A. C.; Neves, M.; Geraldes, C. F. G. C.; Lima, J. J. P. deTwo DTPA derivatives, a mono-amide derivative containing an iodinated synthon, DTPA-IOPsp (L1) and the ligand DTPA(BOM)3 (BOM=benzyloxymethyl) (L2), radiolabelled with 153Sm3+ and 111In3+, were studied as potential hepatospecific gamma scintigraphic agents. In vivo studies with Wistar rats show that the main excretory pathway for all the chelates studied is the hepatobiliary system. The complexes of L2 show eve...
NODAGATOC, a New Chelator-Coupled Somatostatin Analogue Labeled with [67/68Ga] ...
Eisenwiener, Klaus-Peter; Prata, M. I. M.; Buschmann, I.; Zhang, Han-Wen; Santos, A. C.; Wenger, Sandra; Reubi, Jean Claude; Mäcke, Helmut R.A monoreactive NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid) derived prochelator (1-(1-carboxy-3-carbo-tert-butoxypropyl)-4,7-(carbo-tert-butoxymethyl)-1,4,7-triazacyclononane (NODAGA(tBu)3)) was synthesized in five steps with an overall yield of 21%. It is useful for the coupling to the N-terminus of peptides on solid phase and in solution; it was coupled to [Tyr3]-octreotide (TOC) on solid phase, and th...
Characterization of 111In3+ complexes of DTPA amide derivatives: biodistributio...
Prata, M. I. M.; Santos, A. C.; Bligh, S. W. A.; Chowdhury, A. H. M. S.; Geraldes, C. F. G. C.; Lima, J. J. P. deA large series of structurally related diethylenetriaminepentaacetic acid amide derivatives with different structures and lipophilic properties were synthesized and radiolabeled with 111In3+. Two of the more hydrophobic compounds studied ([111In]L9 and [111In]L10) showed high affinity for human serum albumin (HSA). The biodistribution and clearance properties shown by all complexes upon injection in Wistar rats...
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