Topic
Binding potential
About: Binding potential is a research topic. Over the lifetime, 244 publications have been published within this topic receiving 13918 citations.
Papers published on a yearly basis
Papers
TL;DR: Binding potential values were reduced across many of the regions examined, including frontal, temporal, and limbic cortex in both unmedicated and medicated depressed patients compared with healthy volunteers.
Abstract: Background Pharmacological and postmortem investigations suggest that patients with major depressive disorder have alterations in function or density of brain serotonin1A(5-HT1A) receptors. The aim of the present study was to use positron emission tomography with the selective 5-HT1Areceptor antagonist [11C]WAY-100635 to measure 5-HT1Areceptor binding in depressed patients before and during treatment with selective serotonin reuptake inhibitors. Methods Positron emission tomographic scans with [11C]WAY-100635 were performed on 25 patients with major depressive disorder. These included 15 unmedicated depressed patients. Ten of these unmedicated patients were scanned again during selective serotonin reuptake inhibitor treatment. A further 10 patients with major depressive disorder were scanned on one occasion only while taking selective serotonin reuptake inhibitors. Comparisons were made with [11C]WAY-100635 positron emission tomographic scans in 18 healthy volunteer subjects. Region of interest analysis and statistical parametric mapping were performed on binding potential images generated using a reference tissue model. Results Binding potential values were reduced across many of the regions examined, including frontal, temporal, and limbic cortex in both unmedicated and medicated depressed patients compared with healthy volunteers. Binding potential values in medicated patients were similar to those in unmedicated patients. Conclusions Major depressive disorder is associated with a widespread reduction in 5-HT1Areceptor binding. This reduced 5-HT1Areceptor binding was not changed by selective serotonin reuptake inhibitor treatment.
687 citations
TL;DR: The reference tissue model provided estimates of the binding potential with the same sensitivity for detecting changes as those methods that required a metabolite-corrected plasma input function, indicating that for routine analysis of clinical [11C]raclopride studies, no arterial cannulation is required.
Abstract: Five different methods for the estimation of the binding potential, a measure of Bmax/Kd, of [11C]raclopride in human striatum were compared using data from a dose ranging study of the neuroleptic CP-88,059-01. Binding potential was estimated indirectly, from distribution volumes in striatum and cerebellum, using both single- and two-tissue compartment models with a metabolite-corrected plasma curve as input function. The two-tissue compartment model was also used for a direct estimate of the binding potential. In addition, a direct estimate was obtained from the reference tissue compartment model using the cerebellum as indirect input function. Finally, an estimate of binding potential was calculated from the ratio of striatum over cerebellum counts at late times after injection. The estimates of striatum binding potential from all methods, except the direct determination using a two-tissue compartment model with metabolite-corrected plasma input function, correlated with each other. Use of an average metabolite correction resulted in only a small reduction in accuracy in this series of normal subjects. The reference tissue model provided estimates of the binding potential with the same sensitivity for detecting changes as those methods that required a metabolite-corrected plasma input function. This indicates that for routine analysis of clinical [11C]raclopride studies, no arterial cannulation is required. The range of normal values was significantly less variable with the reference tissue method than when simple striatum-to-cerebellum ratios were used.
493 citations
TL;DR: It is demonstrated that SRTM2 should be a useful method to improve the quality of neuroreceptor functional images thanks to the constrained k′2, which showed somewhat larger biases due to violations of the one-compartment model assumption.
Abstract: The Simplified Reference Tissue Model (SRTM) produces functional images of receptor binding parameters using an input function derived from a reference region and assuming a model with one tissue compartment. Three parameters are estimated: binding potential (BP), relative delivery (R1), and the reference region clearance constant k'2. Since k'2 should not vary across brain pixels, the authors developed a two-step method (SRTM2) using a global value of k'2. Whole-brain simulations were performed using human input functions and rate constants for [18F]FCWAY, [11C]flumazenil, and [11C]raclopride, and parameter SD and bias were determined for SRTM and SRTM2. The global mean of k'2 was slightly biased (2% to 6%), but the median was unbiased (<1%) and was used as the global value. Binding potential noise reductions with SRTM2 were 4% to 14%, 20% to 53%, and 10% to 30% for [18F]FCWAY, [11C]flumazenil, and [11C]raclopride, respectively, with larger reductions for shorter scans. R1 noise reduction was larger than that of BP. Simulations were also performed to assess bias when the reference and/or tissue regions followed a two-tissue compartment model. Owing to the constrained k'2, SRTM2 showed somewhat larger biases due to violations of the one-compartment model assumption. These studies demonstrate that SRTM2 should be a useful method to improve the quality of neuroreceptor functional images.
458 citations
TL;DR: Generalized social phobia may be associated with low binding of [(123)I]IBZM to D(2) receptors in the striatum, and there was a nonsignificant correlation of binding potential with the Liebowitz Social Anxiety Scale score.
Abstract: OBJECTIVE: This study compared dopamine D2 receptor binding potential in patients with social phobia and healthy comparison subjects. METHOD: Dopamine D2 receptor binding potential was assessed in 10 unmedicated subjects with generalized social phobia and no significant lifetime psychiatric comorbidity and 10 healthy comparison subjects matched for age and sex. Binding potential was measured in the striatum by using single photon emission computerized tomography and constant infusion of the D2 receptor radiotracer [123I]iodobenzamide ([123I]IBZM). RESULTS: Mean D2 receptor binding potential was significantly lower in the subjects with social phobia than in the comparison subjects. Within the social phobia group, there was a nonsignificant correlation of binding potential with the Liebowitz Social Anxiety Scale score. CONCLUSIONS: Generalized social phobia may be associated with low binding of [123I]IBZM to D2 receptors in the striatum.
336 citations
TL;DR: Factors impacting on the imaging quality that are related to the radiotracer per se are discussed, and it is shown that, within a given structural family, affinity and lipophilicity are associated with scan outcome in a relatively predictable manner.
Abstract: In molecular imaging of the brain, many factors affect the reliability of the quantitative information that can be derived from the imaging process. This article discusses factors impacting on the imaging quality that are related to the radiotracer per se. Following a brief summary of key concepts in receptor quantification, a number of these factors are discussed, including selectivity, affinity, delivery, and lipophilicity. Concepts discussed in the theoretical section are then illustrated, by reviewing a recent comparative evaluation of four agents developed to label the serotonin transporter ([(11)C]ADAM, [(11)C]DASB, [(11)C]DAPA, and [(11)C]AFM). Specifically, the relationship between affinity and lipophilicity, measured in vitro, and several scanning parameters are investigated. These include peripherical metabolism, brain uptake, required scanning time, nonspecific binding, and binding potential. It is shown that, within a given structural family, affinity and lipophilicity are associated with scan outcome in a relatively predictable manner.
260 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2025 | 5 |
| 2024 | 3 |
| 2023 | 26 |
| 2022 | 31 |
| 2021 | 6 |
| 2020 | 7 |