Comparison of [(18)F]altanserin and [(18)F]deuteroaltanserin for PET imaging of serotonin(2A) receptors in baboon brain: pharmacological studies
| Autor: | Ping-Zhong Tan, Pradeep K. Garg, Quinn Ramsby, Chin Ng, Christopher H. van Dyck, Robert B. Innis, Robert Soufer, Mohammed S Al Tikriti, Julie K. Staley, Heide Klump, Ronald M. Baldwin |
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| Rok vydání: | 2001 |
| Předmět: |
Cancer Research
medicine.medical_specialty Fluorine Radioisotopes Fenfluramine medicine.drug_class chemistry.chemical_compound Internal medicine biology.animal medicine Animals Radiology Nuclear Medicine and imaging Receptor 5-HT receptor Analysis of Variance Radiochemistry biology Chemistry Binding potential Brain Receptor antagonist Deuterium Endocrinology Receptors Serotonin Altanserin Molecular Medicine Female Serotonin Ketanserin medicine.drug Baboon Papio Tomography Emission-Computed |
| Zdroj: | Nuclear medicine and biology. 28(3) |
| ISSN: | 0969-8051 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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