| Literature DB >> 11323237 |
J K Staley1, C H Van Dyck, P Z Tan, M Al Tikriti, Q Ramsby, H Klump, C Ng, P Garg, R Soufer, R M Baldwin, R B Innis.
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.Entities:
Mesh：
Substances：
Year: 2001 PMID： 11323237 DOI： 10.1016/s0969-8051(00)00212-2
Source DB: PubMed Journal: Nucl Med Biol ISSN： 0969-8051 Impact factor: 2.408