Ograniczanie wyników
Preferencje help
Widoczny [Schowaj] Abstrakt
Liczba wyników

Znaleziono wyników: 2

Liczba wyników na stronie
first rewind previous Strona / 1 next fast forward last
Wyniki wyszukiwania
Wyszukiwano:
w słowach kluczowych:  benzovisamicol derivatives
help Sortuj według:

help Ogranicz wyniki do:
first rewind previous Strona / 1 next fast forward last
EN
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.
EN
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.
first rewind previous Strona / 1 next fast forward last
JavaScript jest wyłączony w Twojej przeglądarce internetowej. Włącz go, a następnie odśwież stronę, aby móc w pełni z niej korzystać.