Substituted benzamides as ligands for visualization of dopamine receptor binding in the human brain by positron emission tomography.

Farde, Lars; Ehrin, E.; Eriksson, Lars; Greitz, T.; Hall, Håkan; Hedström, Carl-Göran; Litton, Jan-Erik; Sedvall, Göran

doi:10.1073/pnas.82.11.3863

Cited by 283 publications

(119 citation statements)

References 23 publications

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“…The reference method assumes that nonspecific binding of the tracer is equivalent in the striatum and reference region. Raclopride has been shown to have negligible nonspecific binding (Farde et al, 1985). We have demonstrated that this method is insensitive to changes in cerebral blood flow (Aston et al, 2000).…”

Section: Pet Proceduresmentioning

confidence: 83%

Stress-Induced Dopamine Release in Humans at Risk of Psychosis: a [11C]Raclopride PET Study

Soliman

O’Driscoll

Pruessner

et al. 2007

Neuropsychopharmacol

133

109

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Drugs that increase dopamine levels in the brain can cause psychotic symptoms in healthy individuals and worsen them in schizophrenic patients. Psychological stress also increases dopamine release and is thought to play a role in susceptibility to psychotic illness. We hypothesized that healthy individuals at elevated risk of developing psychosis would show greater striatal dopamine release than controls in response to stress. Using positron emission tomography and [ 11 C]raclopride, we measured changes in synaptic dopamine concentrations in 10 controls and 16 psychometric schizotypes; 9 with perceptual aberrations (PerAb, ie positive schizotypy) and 7 with physical anhedonia (PhysAn, ie negative schizotypy). [ 11 C]Raclopride binding potential was measured during a psychological stress task and a sensory-motor control. All three groups showed significant increases in self-reported stress and cortisol levels between the stress and control conditions. However, only the PhysAn group showed significant stress-induced dopamine release. Dopamine release in the entire sample was significantly negatively correlated with smooth pursuit gain, an endophenotype linked to frontal lobe function. Our findings suggest the presence of abnormalities in the dopamine response to stress in negative symptom schizotypy, and provide indirect evidence of a link to frontal function.

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Section: Pet Proceduresmentioning

confidence: 83%

Stress-Induced Dopamine Release in Humans at Risk of Psychosis: a [11C]Raclopride PET Study

Soliman

O’Driscoll

Pruessner

et al. 2007

Neuropsychopharmacol

133

109

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“…Research on the development of more spe cific Dz ligands has shown the potential of other series of dopamine antagonists, such as benzamide and ergolene analogues. Among the benzamides, raclopride was labeled with IIC and successfully used for the selective analysis by positron emission tomography (PET) of central Dz receptors in pri mates and humans (Farde et al, 1985). Among the ergolene derivatives, 2-bromolisuride (BLIS) has specific antidopaminergic properties.…”

Section: Discussionmentioning

confidence: 99%

Kinetic Analysis of Central [⁷⁶Br]Bromolisuride Binding to Dopamine D₂ Receptors Studied by PET

Delforge

Loc’h

Hantraye

et al. 1991

J Cereb Blood Flow Metab

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Summary:The in vivo kinetic analysis of dopamine D 2 receptors was obtained in baboon brain using positron emission tomography (PET) and C6Brjbromolisuride W6BrjBLlS) as radioligand. An injection of a trace amount of C6BrjBLlS was followed 3 h later by an injec tion of a mixture of C6BrjBLlS and BLIS in the same syringe (coinjection experiment). A third injection per formed at 6 h was either an excess of unlabeled ligand (displacement experiment) or a second coinjection. This protocol allowed us to evaluate in the striatum of each animal and after a single experiment the quantity of avail able receptors (B:naJ and the kinetic parameters includ ing the association and dissociation rate constants (k + I V R and k _ l' respectively, where V R is the volume of reac tion). The cerebellum data were fitted using a model with out specific binding. All the parameters were estimatedThe dopaminergic system was the first neuro transmission system in which it was possible to im age receptors, stored neurotransmitters, and neuro transmitter reuptake mechanisms. For a long time, most researchers endorsed the hypothesis that there were at least two major dopamine receptor types: DJ receptors linked to the stimulation of ade nylate cyclase and D2 receptors linked to the inhi bition of this enzyme (Kebabian and CaIne, 1979 Abbreviations used: BLIS, bromolisuride ; PET, po sitron emission tomography; ROI, region of interest; TLC, thin layer chromatography. 914using nonlinear mathematical models of the ligand receptor interactions including or not including nonspe cific binding. The plasma time-concentration curve was used as an input function after correction for the metab olites. An estimate of standard errors was obtained for each PET study and for each identified parameter using the covariance matrix. The average values of B:n ax and Kd V R were 73 ± II pmollml tissue and 1.9 ± 0.9 pmollml, respectively. The nonspecific binding was identifiable in the experiment where the last injection corresponded to a second coinjection. We found that �6% of the striatal binding was nonspecific after a tracer injection of C6Brj BLIS. The nonspecific binding appeared to be reversible in the striatum but irreversible in the cerebellum.

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“…11 C]SCH23390 (Halldin et al, 1986;Farde et al, 1987) and [ 11 C]raclopride (Farde et al, 1985;Köhler et al, 1985;Ito et al, 1998), respectively. The relative activity of cerebral aromatic L-amino acid decarboxylase (AADC) representing endogenous dopamine synthesis rate measured by 6-[…”

Section: Introductionmentioning

confidence: 99%

Relation between Presynaptic and Postsynaptic Dopaminergic Functions Measured by Positron Emission Tomography: Implication of Dopaminergic Tone

Ito¹,

Kodaka²,

Takahashi³

et al. 2011

J. Neurosci.

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Both presynaptic and postsynaptic dopaminergic functions can be estimated by positron emission tomography (PET). While both presynaptic and postsynaptic dopaminergic functions would be regulated by corresponding genes and related to personality traits, the relation between presynaptic and postsynaptic functions in terms of interindividual variation has hardly been investigated. In the present study, both striatal dopamine D 2 receptor binding and endogenous dopamine synthesis rate were measured in the same healthy subjects using PET with [

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Substituted benzamides as ligands for visualization of dopamine receptor binding in the human brain by positron emission tomography.

Cited by 283 publications

References 23 publications

Stress-Induced Dopamine Release in Humans at Risk of Psychosis: a [11C]Raclopride PET Study

Stress-Induced Dopamine Release in Humans at Risk of Psychosis: a [11C]Raclopride PET Study

Kinetic Analysis of Central [⁷⁶Br]Bromolisuride Binding to Dopamine D₂ Receptors Studied by PET

Relation between Presynaptic and Postsynaptic Dopaminergic Functions Measured by Positron Emission Tomography: Implication of Dopaminergic Tone

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Substituted benzamides as ligands for visualization of dopamine receptor binding in the human brain by positron emission tomography.

Cited by 283 publications

References 23 publications

Stress-Induced Dopamine Release in Humans at Risk of Psychosis: a [11C]Raclopride PET Study

Stress-Induced Dopamine Release in Humans at Risk of Psychosis: a [11C]Raclopride PET Study

Kinetic Analysis of Central [76Br]Bromolisuride Binding to Dopamine D2 Receptors Studied by PET

Relation between Presynaptic and Postsynaptic Dopaminergic Functions Measured by Positron Emission Tomography: Implication of Dopaminergic Tone

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Kinetic Analysis of Central [⁷⁶Br]Bromolisuride Binding to Dopamine D₂ Receptors Studied by PET