Comparison of [(18)F]altanserin and [(18)F]deuteroaltanserin for PET imaging of serotonin(2A) receptors in baboon brain: pharmacological studies.
Nucl Med Biol
; 28(3): 271-9, 2001 Apr.
Article
en En
| MEDLINE
| ID: mdl-11323237
ABSTRACT
The regional distribution in brain, distribution volumes, and pharmacological specificity of the PET 5-HT(2A) receptor radiotracer [(18)F]deuteroaltanserin were evaluated and compared to those of its non-deuterated derivative [(18)F]altanserin. Both radiotracers were administered to baboons by bolus plus constant infusion and PET images were acquired up to 8 h. The time-activity curves for both tracers stabilized between 4 and 6 h. The ratio of total and free parent to metabolites was not significantly different between radiotracers; nevertheless, total cortical R(T) (equilibrium ratio of specific to nondisplaceable brain uptake) was significantly higher (34-78%) for [(18)F]deuteroaltanserin than for [(18)F]altanserin. In contrast, the binding potential (Bmax/K(D)) was similar between radiotracers. [(18)F]Deuteroaltanserin cortical activity was displaced by the 5-HT(2A) receptor antagonist SR 46349B but was not altered by changes in endogenous 5-HT induced by fenfluramine. These findings suggest that [(18)F]deuteroaltanserin is essentially equivalent to [(18)F]altanserin for 5-HT(2A) receptor imaging in the baboon.
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Base de datos:
MEDLINE
Asunto principal:
Ketanserina
/
Encéfalo
/
Radioisótopos de Flúor
/
Tomografía Computarizada de Emisión
/
Receptores de Serotonina
Límite:
Animals
Idioma:
En
Revista:
Nucl Med Biol
Asunto de la revista:
BIOLOGIA
/
MEDICINA NUCLEAR
Año:
2001
Tipo del documento:
Article
País de afiliación:
Estados Unidos