Synthesis and biodistribution of R- and S-isomers of [18F]-fluoropropranolol, a lipophilic ligand for the beta-adrenergic receptor.
Nucl Med Biol
; 26(8): 891-6, 1999 Nov.
Article
en En
| MEDLINE
| ID: mdl-10708302
ABSTRACT
The S and R isomers of [18F]-fluoropropranolol (1-[1-fluoro-2-isopropylamino]-3-naphthalen-1-yloxy-propan-2 -ol) have been prepared by reductive alkylation of the appropriate aminoalcohols. The radiosynthesis provides a reasonable yield (approximately 25%) to give products of 99% enantiomeric excess and specific activities of 1-3 Ci/micromol. The dissociation constants for the beta2 adrenergic receptor are 0.5 and 2.5 nM for the S and the R isomers, respectively. The biodistribution data in rats show that uptake and egress of the tracer is rapid but that the result of blocking studies and the difference between the R and the S isomers suggest receptor-mediated uptake in receptor-rich tissue.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Propranolol
/
Receptores Adrenérgicos beta
/
Radiofármacos
Límite:
Animals
Idioma:
En
Revista:
Nucl Med Biol
Asunto de la revista:
BIOLOGIA
/
MEDICINA NUCLEAR
Año:
1999
Tipo del documento:
Article
País de afiliación:
Estados Unidos