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1.
Phys Rev Lett ; 105(25): 252501, 2010 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-21231582

RESUMO

The "island of inversion" nucleus 32 Mg has been studied by a (t, p) two neutron transfer reaction in inverse kinematics at REX-ISOLDE. The shape coexistent excited 0+ state in 32 Mg has been identified by the characteristic angular distribution of the protons of the Δ L=0 transfer. The excitation energy of 1058 keV is much lower than predicted by any theoretical model. The low γ-ray intensity observed for the decay of this 0+ state indicates a lifetime of more than 10 ns. Deduced spectroscopic amplitudes are compared with occupation numbers from shell-model calculations.

2.
Bioorg Med Chem Lett ; 19(3): 602-5, 2009 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-19147351

RESUMO

2-(4'-[(18)F]fluorophenyl)-1,3-benzothiazole was synthesized as a fluorine-18 labelled derivative of the Pittsburg Compound-B (PIB), which has known affinity for amyloid beta and promising characteristics as tracer for in vivo visualisation of amyloid deposits in patients suffering from Alzheimer's disease (AD). Both the nitro-precursor 2-(4'-nitrophenyl)-1,3-benzothiazole and the non-radioactive reference compound were synthesized using a 1-step synthesis pathway. Labelling was achieved by direct aromatic nucleophilic substitution of the nitro-precursor using [(18)F]fluoride by heating for 20 min at 150 degrees C and with a radiochemical yield of 38%. The reference compound showed high affinity for amyloid in an in vitro competition binding study using human AD brain homogenates (K(i)=9.0 nM) and fluorescence imaging of incubated transgenic APP mouse brain slices confirmed binding to amyloid plaques. A biodistribution study in normal mice showed a high brain uptake at 2 min pi (3.20%ID/g) followed by a fast washout (60 min pi: 0.21%ID/g). A dynamic microPET study was performed in a transgenic APP and normal WT mouse, but, similar to [(11)C]PIB, no difference was seen in tracer retention between both kind of mice. The new (18)F-labelled 2-phenylbenzothiazole showed excellent preclinical characteristics comparable with those of the (11)C-labelled PIB.


Assuntos
Benzotiazóis/química , Química Farmacêutica/métodos , Radioisótopos de Flúor/química , Doença de Alzheimer/tratamento farmacológico , Amiloide/química , Precursor de Proteína beta-Amiloide/genética , Precursor de Proteína beta-Amiloide/metabolismo , Animais , Benzotiazóis/síntese química , Desenho de Fármacos , Humanos , Cinética , Camundongos , Camundongos Transgênicos , Modelos Químicos , Temperatura , Distribuição Tecidual
3.
Br J Cancer ; 91(11): 1947-54, 2004 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-15520822

RESUMO

This study aimed to evaluate tumour hypoxia by comparing [(18)F]Fluoromisonidazole uptake measured using positron emission tomography ([(18)F]FMISO-PET) with immunohistochemical (IHC) staining techniques. Syngeneic rhabdomyosarcoma (R1) tumour pieces were transplanted subcutaneously in the flanks of WAG/Rij rats. Tumours were analysed at volumes between 0.9 and 7.3 cm(3). Hypoxic volumes were defined using a 3D region of interest on 2 h postinjection [(18)F]FMISO-PET images, applying different thresholds (1.2-3.0). Monoclonal antibodies to pimonidazole (PIMO) and carbonic anhydrase IX (CA IX), exogenous and endogenous markers of hypoxia, respectively, were used for IHC staining. Marker-positive fractions were microscopically measured for each tumour, and hypoxic volumes were calculated. A heterogeneous distribution of hypoxia was observed both with histology and [(18)F]FMISO autoradiography. A statistically significant correlation (P<0.05) was obtained between the hypoxic volumes defined with [(18)F]FMISO-PET and the volumes derived from the PIMO-stained tumour sections (r=0.9066; P=0.0001), regardless of the selected threshold between 1.4 and 2.2. A similar observation was made with the CA IX staining (r=0.8636; P=0.0006). The relationship found between [(18)F]FMISO-PET and PIMO- and additionally CA IX-derived hypoxic volumes in rat rhabdomyosarcomas indicates the value of the noninvasive imaging method to measure hypoxia in whole tumours.


Assuntos
Hipóxia Celular , Fluordesoxiglucose F18 , Misonidazol/análogos & derivados , Tomografia por Emissão de Pósitrons , Rabdomiossarcoma/diagnóstico por imagem , Animais , Anticorpos Monoclonais , Anidrase Carbônica III/imunologia , Anidrase Carbônica III/metabolismo , Fluordesoxiglucose F18/farmacocinética , Coração/fisiologia , Técnicas Imunoenzimáticas , Pulmão/metabolismo , Masculino , Músculos/metabolismo , Nitroimidazóis/imunologia , Nitroimidazóis/metabolismo , Radiossensibilizantes , Compostos Radiofarmacêuticos/farmacocinética , Ratos , Rabdomiossarcoma/metabolismo , Rabdomiossarcoma/patologia
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