Effects of cocaine on [11C]norepinephrine and [11C]β-CIT uptake in the primate peripheral organs measured by PET

Suhara, Tetsuya; Farde, Lars; Halldin, Christer; Någren, Kjell; Karlsson, Per

doi:10.1007/bf03165058

Cited by 8 publications

(6 citation statements)

References 16 publications

(6 reference statements)

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“…However, a recent study indicated that there was no firm relation between logP values of the compounds and the degree of non-specific binding in PET/SPET studies [34]. For the quantification of these ligands, compartment model-based methods would be required that include the effects of prolonged input and high non-specific binding [35]; the peripheral uptake of radioligands might be an important factor to be considered in the development of ligands, such as 5-HT transporter ligands [36,37].…”

Section: Discussionmentioning

confidence: 98%

Comparative evaluation of two serotonin transporter ligands in the human brain: [11C](+)McN5652 and [11C]cyanoimipramine

Takano¹,

Suhara²,

Sudo³

et al. 2002

Eur J Nucl Med

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Serotonin (5-HT) is considered to be an important transmitter underlying mood and behaviour. Abnormalities of the 5-HT transporter have been suggested in mood disorders, since it is one of the major binding sites of antidepressants. A number of ligands have been developed to visualise the 5-HT transporter in vivo, but only a few have successfully visualised specific binding in vivo. In this study, we comparatively evaluated two ligands for 5-HT transporter, [(11)C](+)McN5652 and [(11)C]cyanoimipramine, in the human brain. Brain uptake of [(11)C](+)McN5652 and [(11)C]cyanoimipramine was measured with PET in 15 healthy volunteers. Second PET scans were performed after pretreatment with the potent 5-HT reuptake inhibitor clomipramine. Data were analysed as regional brain uptake as well as whole brain uptake. In six healthy volunteers uptake of the two ligands was also measured in the lung since it is one of the high-uptake organs in the body. In the brain, high accumulation was observed in the thalamus and striatum, the regions known to contain high densities of 5-HT transporter, for both [(11)C](+)McN5652 and [(11)C]cyanoimipramine. The average ratio of thalamus to cerebellum uptake at 90 min after the tracer injection was approximately 1.6 for [(11)C](+)McN5652 and 1.7 for [(11)C]cyanoimipramine, while the ratios obtained after pretreatment with clomipramine were approximately 1.2. However, the whole brain uptake of [(11)C](+)McN5652 was approximately twice that of [(11)C]cyanoimipramine, while the lung uptake of [(11)C](+)McN5652 was approximately half that of [(11)C]cyanoimipramine. Both [(11)C](+)McN5652 and [(11)C]cyanoimipramine showed sufficient specific binding for performance of a quantitative analysis in the brain. [(11)C](+)McN5652 could be superior because of its higher distribution to the brain.

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Section: Discussionmentioning

confidence: 98%

Comparative evaluation of two serotonin transporter ligands in the human brain: [11C](+)McN5652 and [11C]cyanoimipramine

Takano¹,

Suhara²,

Sudo³

et al. 2002

Eur J Nucl Med

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“…Human aging is also associated with elevated activation of the sympathetic nervous system and stress response [59], primarily through decreased norepinephrine reuptake [60,61]. For instance, as a robust modulator of monoamine transmission, cocaine also alters both central and peripheral norepinephrine function [13,62,63]. Cocaine is also a sigma-1 receptor agonist, acting on various leukocyte populations [64].…”

Section: Discussionmentioning

confidence: 99%

Elevated Neutrophil to Lymphocyte Ratio in Older Adults with Cocaine Use Disorder as a Marker of Chronic Inflammation

Soder¹,

Berumen²,

Gomez³

et al. 2020

Clin Psychopharmacol Neurosci

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Objective: The neutrophil to lymphocyte ratio (NLR) is a non-specific, easy-to-obtain marker of inflammation associated with morbidity and mortality in systemic, psychiatric, and age-related inflammatory conditions. Given the growing trend of substance use disorder (SUD) in older adults, and the relationship between inflammation and SUD elevated NLR may serve as a useful inflammatory biomarker of the combined burden of aging and SUD. The present study focused on cocaine use disorder (CUD) to examine if cocaine adds further inflammatory burden among older adults, by comparing NLR values between older adults with CUD and a non-cocaine using, aged-matched, nationally representative sample. Methods: The dataset included 107 (86% male) participants (aged 50−65 years) with cocaine use disorder. NLR was derived from complete blood count tests by dividing the absolute value of peripheral neutrophil concentration by lymphocyte concentration. For comparison, we extracted data from age-matched adults without CUD using the National Health and Nutrition Examination Survey. Individuals with immunocompromising conditions were excluded (e.g., rheumatoid arthritis and sexually transmitted infections such as HIV). A doubly-robust inverse probability-weighted regression adjustment (IPWRA) propensity score method was used to estimate group differences on NLR while controlling for potential confounding variables (age, gender, race, income, nicotine, marijuana and alcohol use). Results: The IPWRA model revealed that the CUD sample had significantly elevated NLR in comparison to non-cocaine users, with a moderate effect size ( weight = 0.67). Conclusion: Although non-specific, NLR represents a readily obtainable inflammatory marker for SUD research. CUD may add further inflammatory burden to aging cocaine users.

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“…642,683 Both desipramine and cocaine had a negative effect on [ 11 C]norepinephrine retention in the heart (−80% with desipramine and −33% with cocaine). 642,683 Metabolite studies were also performed in cynomolgus monkeys. [ 11 C]Norepinephrine showed a high metabolic resistance in the plasma, with 90% of the parent molecule remaining intact at 30 min after the tracer injection.…”

Section: Radiosynthesismentioning

confidence: 99%

“…Other in vivo studies focused on how pharmacological agents affect the pharmacokinetics of [ 11 C]norepinephrine. In particular, the effect of desipramine (inhibitor of the norepinephrine reuptake transporter) and cocaine on [ 11 C]norepinephrine biodistribution was investigated in cynomolgus monkeys. , Both desipramine and cocaine had a negative effect on [ 11 C]norepinephrine retention in the heart (−80% with desipramine and −33% with cocaine). , …”

Section: Hormones and Neurotransmittersmentioning

confidence: 99%

Radiosynthesis, Preclinical, and Clinical Positron Emission Tomography Studies of Carbon-11 Labeled Endogenous and Natural Exogenous Compounds

et al. 2022

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The presence of positron emission tomography (PET) centers at most major hospitals worldwide, along with the improvement of PET scanner sensitivity and the introduction of total body PET systems, has increased the interest in the PET tracer development using the short-lived radionuclides carbon-11. In the last few decades, methodological improvements and fully automated modules have allowed the development of carbon-11 tracers for clinical use. Radiolabeling natural compounds with carbon-11 by substituting one of the backbone carbons with the radionuclide has provided important information on the biochemistry of the authentic compounds and increased the understanding of their in vivo behavior in healthy and diseased states. The number of endogenous and natural compounds essential for human life is staggering, ranging from simple alcohols to vitamins and peptides. This review collates all the carbon-11 radiolabeled endogenous and natural exogenous compounds synthesised to date, including essential information on their radiochemistry methodologies and preclinical and clinical studies in healthy subjects.

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Effects of cocaine on [11C]norepinephrine and [11C]β-CIT uptake in the primate peripheral organs measured by PET

Cited by 8 publications

References 16 publications

Comparative evaluation of two serotonin transporter ligands in the human brain: [11C](+)McN5652 and [11C]cyanoimipramine

Comparative evaluation of two serotonin transporter ligands in the human brain: [11C](+)McN5652 and [11C]cyanoimipramine

Elevated Neutrophil to Lymphocyte Ratio in Older Adults with Cocaine Use Disorder as a Marker of Chronic Inflammation

Radiosynthesis, Preclinical, and Clinical Positron Emission Tomography Studies of Carbon-11 Labeled Endogenous and Natural Exogenous Compounds

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