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    Wyświetlanie 1-4 z 4
    Tytuł:
    Radiosynthesis and biological evaluation of 123I-(±)-trans-2-hydroxy-5-((E)- -3-(iodo)allyloxy)-3-(4-phenyl-1-piperazinyl) tetralin
    Autorzy:
    Assaad, T.
    Al Rayyes, A. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/147888.pdf
    Data publikacji:
    2012
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    Alzheimer's disease
    brain biodistribution
    injected dose (ID)
    radioiodination
    vesamicol derivatives
    vesicular acetylcholine transporter (VAChT)
    Opis:
    This work reports both the radiolabeling and preliminary biodistribution results in the rat brains of (±)-[123I]- -II. The novel benzovesamicol derivative (±)-[123I]-II was successfully labeled with iodine-123 from its corresponding n-tributyltin, with radiochemical purity greater than 97% and radiochemical yield in the range 50–55%. (±)-[123I]-II showed a higher accumulation in striatum than in the other regions studied. To determine if (±)-[123I]-II could provide an advantage compared to reference compound [125I]-IBVM a kinetic study was carried out, at each point of the kinetic study, (±)-[123I]-II showed a lower specific binding compared to [125I]-IBVM. Time activity curves of (±)-[123I]-II confirmed that this compound is inferior to [125I]-IBVM to explore the VAChT in vivo by SPECT. Moreover, it is well known that interaction at the VAChT binding site is enantioselective, and therefore, working with enantiomerically pure compounds, could improve the compound activity.
    Źródło:
    Nukleonika; 2012, 57, 1; 75-80
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and biodistribution of both (±)-5-[ 18F]-fluoroethoxy and (±)-5-[ 18F]-fluoropropoxy piperazine analogs of benzovesamicol as vesicular acetylcholine transporter ligands (VAChT)
    Autorzy:
    Assaad, T.
    Al Rayyes, A. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/147599.pdf
    Data publikacji:
    2013
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    Alzheimer's disease (AD)
    benzovisamicol derivatives
    brain biodistribution
    enantiomeric resolution
    radiofluorination
    vesicular acetylcholine transporter (VAChT)
    Opis:
    The radiosynthesis and preliminary biological evaluation in rats’ brain of two novel piperazine analogs of benzovesamicol as ligands for the vesicular acetylcholine transporter (VAChT) have been carried out. The novel benzovesamicol derivatives 5-(2-fluoroethoxy)-3-(4-phenylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-ol and 5-(3-fluoropropoxy)-3-(4-phenylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-ol [(±)-[18F]-6 and (±)-[18F]-7] were successfully labelled with fluorine-18 from their tosylate precursors, with radiochemical purities greater than 98% and with radiochemical yield in the range of 5–6%. To determine whether these compounds could have potential advantage compared to [125I]-iodo benzovesamicol (IBVM), IBVM was also labelled and used as the reference compound in all in vivo experiments. Both (±)-[18F]-6 and (±)-[18F]-7 showed lower specific binding in all brain areas explored 2 h post injection when compared to reference compound (-)-[125I] IBVM. Furthermore, defluorination indicated that (±)-[18F]-6 and (±)-[18F]-7 are not suitable as radioligands to explore the VAChT in vivo by PET. Moreover, it is well known that interaction at the VAChT binding site is enantioselective, and therefore, working with enantiomerically pure compounds, could improve the compound activity.
    Źródło:
    Nukleonika; 2013, 58, 2; 269-274
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and in vivo evaluation of both (2R,3R)-[123I]- and (2S,3S)- -[123I]-trans-2-hydroxy-5-((E)-3-(iodo) allyloxy)-3-(4-phenyl-1-piperazinyl) tetralin as SPECT radiotracer
    Autorzy:
    Assaad, T.
    Al Rayyes, A. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/148128.pdf
    Data publikacji:
    2013
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    Alzheimer's disease
    benzovisamicol derivatives
    brain biodistribution
    enantiomeric resolution
    radioiodination
    vesicular acetylcholine transporter (VAChT)
    Opis:
    We report the synthesis of enantiopure benzovesamicol derivatives: (2R,3R)-[123I]-trans-2-hydroxy-5-((E)-3- -(iodo)allyloxy)-3-(4-phenyl-1-piperazinyl) tetralin and (2S,3S)-[123I]-trans-2-hydroxy-5-((E)-3-(iodo)allyloxy)-3-(4- phenyl-1-piperazinyl) tetralin; [(2R,3R)-[123I]-1 and (2S,3S)-[123I]-1]. Both compounds were obtained with radiochemical and optical purities greater than 97% and with radiochemical yields in the range of 50–60%. To determine whether these compounds could have potential advantage compared to [125I]-iodo benzovesamicol (IBVM), IBVM was also labelled and used as the reference compound in all in vivo experiments. Both (2R,3R)-[123I]-1 and (-)-[125I]-IBVM showed similar time activity curves (TACs) with the highest accumulations in the striatum region followed by the cortex, hippocampus and then cerebellum. While (2S,3S)-[123I]-1 showed an overall homogeneous brain distribution. However, time activity curves of (2R,3R)-[123I]-1 confirmed that this compound could be used to visualize the vesicular acetylcholine transporter (VAChT) in vivo, at each point of the kinetic study. Also (2R,3R)-[123I]-1 showed lower specific bindings compared to [125I]-IBVM. These results suggested that (2R,3R)-[123I]-1 is inferior in comparison with [125I]-IBVM for in vivo VAChT exploration.
    Źródło:
    Nukleonika; 2013, 58, 2; 261-267
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    New microwave assisted radiolabelling method and rat brain biodistribution study of two new 99mTc-tricarbonyl complexes as potential brain imaging agents
    Autorzy:
    Trabelsi, M.
    Mekni, A.
    Solanki, Ch.
    Maltby, P.
    Saidi, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/147766.pdf
    Data publikacji:
    2008
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Opis:
    Two new cyclopentadienyl piperidine derivatives, namely ferrocene carboxylic acid 1-ethyl-3-hydroxypiperidinyl ester and ferrocene carboxylic acid 4-hydroxypiperidinyl ester, were synthesized. The ligands were then radiolabelled with 99mTc using two different approaches. The first method consisted of reacting the ligand precursor with Mn(CO)5Br in pertechnetate 99mTcO4 - in normal saline and dimethyl formamide (DMF) at 150°C for 1 h. The yields were 70% and 90%, respectively. For the second method, the reactions mixtures were placed in a microwave oven for 2 min at 650 watt. The yields were higher than 90% for both 99mTc complexes. Biodistribution studies showed that tricarbonyl{eta5- [carboxy-3-hydroxy(N-ethyl)piperidine]cyclopentadienyl}technetium(I) had the highest brain uptake. The regional distribution in the brain also demonstrated relatively higher uptake of tricarbonyl{eta5-[carboxy-3-hydroxy(N-ethyl) piperidine]cyclopentadienyl}technetium(I) in the colliculus (1.97% ID/g tissue,) with the colliculus to cerebellum ratio of 1.99. We conclude that the radiolabelling can be achieved by microwave activation, and tricarbonyl{eta5-[carboxy-3- hydroxy(N-ethyl)piperidine]cyclopentadienyl}technetium(I) has the potential for use as central nervous system (CNS) imaging agent.
    Źródło:
    Nukleonika; 2008, 53, 3; 97-101
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-4 z 4

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