N-methylpiperidinemethyl, N-methylpyrrolidyl and N-methylpyrrolidinemethyl esters as PET radiotracers for acetylcholinesterase activity.
Nucl Med Biol
; 30(3): 293-302, 2003 Apr.
Article
en En
| MEDLINE
| ID: mdl-12745021
The N-[(11)C]methylpiperidinyl esters are used as radiopharmaceuticals for measuring brain cholinesterase activity. We have synthesized a series of N-methylpiperidinemethyl (1), N-methylpyrrolidinyl (2) and N-methylpyrrolidinemethyl (3) esters and examined the effects of sterric constraint and stereochemistry on cholinesterase-mediated cleavage. Acetylcholinesterase exhibited a preference for primary esters 1 and for the R-isomers of both 1 and 2. Biological data for (S)-N-[(11)C]methyl-2-piperidinemethyl acetate (1a) were similar to [(11)C]AMP. These data better define the structure-activity relationships for cholinesterase radiotracers and provide lead compounds for (18)F- labeling.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Piperidinas
/
Acetilcolinesterasa
/
Pirrolidinas
/
Encéfalo
/
Radiofármacos
Límite:
Animals
Idioma:
En
Revista:
Nucl Med Biol
Asunto de la revista:
BIOLOGIA
/
MEDICINA NUCLEAR
Año:
2003
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Estados Unidos