ISSN:
1619-7089
Keywords:
S2 serotonin receptors
;
Fluoroethylspiperone
;
Positron emission tomography
;
Neuroreceptor modelling
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract We used the ligand 3-N-(2′-F 18)fluoroethylspiperone (FESP) and positron emission tomography (PET) to quantify in vivo serotonin S2 neuroreceptor density and affinity in the baboon frontal cortex. In the cortex, FESP binds specifically and exclusively to S2 receptors, and an equilibrium is reached when the rate of ligand-receptor association and dissociation become equal. Using multiple studies in the same baboon, an equilibrium (saturation) analysis approach provided a linear Hill plot with a slope of 1.02 (r 2 =0.988,P 〈0.0001), indicative of ligand binding to a single receptor class. Using serial PET scans, a dynamic approach was also used to quantify S2 receptors in the frontal cortex of the baboon, which provided an estimate of receptor densityB max =35.6 ± 10.9 pmol/g. The rate constants corresponding to transport into and out of tissue wereK * 1 = 0.2720 ± 0.0299 mol/min ⁗ g andk * 2 = 0.0786 ± 0.0315 min−1, respectively. The ligand-receptor dissociation constant wask * 4 = 0.0154 ± 0.0109 min−1.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02262725
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