Preparation and biodistribution of [125I]IBZM: A potential CNS D-2 dopamine receptor imaging agent

Kung, Hank F.; Guo, Yanbao; Billings, J.; Xu, Xiaohui; Mach, Robert H.; Blau, Monte; Ackerhalt, R.

doi:10.1016/0883-2897(88)90088-8

Cited by 75 publications

(54 citation statements)

References 9 publications

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“…In PET and SPECT studies in primates and humans increases in the levels of synaptic dopamine produced by administration of either amphetamine or dopamine uptake inhibitors such as cocaine and methylphenidate have similarly been found to produce modest decreases (10-40%) in the binding of [ 11 C]raclopride and or of [ 123 I]IBZM (Innis et al 1992;Volkow et al 1994;Laruelle et al 1995;Carson et al 1997;Laruelle et al 1997;Volkow et al 1999). One frequent observation that has arisen from studies on the effects of changes in dopamine on radiotracer binding in rodent and primate PET studies is that the lower affinity radiotracers, such as raclopride and IBZM (K d of 0.4-1 nM; Kung et al 1989;Ross and Jackson 1989a), appear to be more susceptible to competition by synaptic dopamine than other D 2 radiotracers such as epidepride and N-methylspiperone, which have very high receptor affinities (K d Ͻ 0.1 nM). D 1 receptors have been less frequently investigated in imaging studies than D 2 receptors.…”

mentioning

confidence: 99%

Effects of Endogenous Neurotransmitters on the in vivo Binding of Dopamine and 5-HT Radiotracers in Mice

Rice

2001

Neuropsychopharmacology

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confidence: 99%

Effects of Endogenous Neurotransmitters on the in vivo Binding of Dopamine and 5-HT Radiotracers in Mice

Rice

2001

Neuropsychopharmacology

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“…123 I]IBZM, 0.4 nM (Kung et al, 1989), permits accurate measurement of DA D 2 receptor levels only in the striatum, which has the highest DA D 2 receptor levels in brain (Kessler et al, 1993b;Laruelle et al, 1995;Drevets et al, 2001). With the development of high-affinity radioligands, such as [ (Kessler et al, 1991(Kessler et al, , 1992(Kessler et al, , 1993aHalldin et al, 1995;Mukherjee et al, 1995).…”

Section: Introductionmentioning

confidence: 99%

Amphetamine-Induced Displacement of [18F] Fallypride in Striatum and Extrastriatal Regions in Humans

Riccardi

Ansari

et al. 2005

Neuropsychopharmacol

125

112

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This study examined D-amphetamine (D-AMPH)-induced displacements of [18 F] fallypride in striatal and extrastriatal regions and the correlations of these displacements with cognition, affect, and sensation-seeking behavior. In all, 14 normal subjects, six females and eight males (ages 21-32, mean age 25.9 years), underwent positron emission tomography (PET) with [18 F]fallypride before and 3 h after a 0.43 mg/kg oral dose of D-AMPH. Levels of dopamine (DA) D 2 receptor density were calculated with the reference region method of Lammerstma. Percent displacements in striatal and extrastriatal regions were calculated for the caudate, putamen, ventral striatum, medial thalamus, amygdala, substantia nigra, and temporal cortex. Correlations of changes in cognition, affect, and sensation seeking with parametric images of D-AMPH-induced DA release were computed. Significant displacements were seen in the caudate, putamen, ventral striatum substantia nigra, and temporal cortex with a trend level change in the amygdala. Greatest displacements were seen in striatal subdivisionsF5.6% in caudate, 11.2% in putamen, 7.2% in ventral striatum, and 6.6% in substantia nigra. Lesser decrements were seen in amygdalaF4.4%, temporal cortexF3.7%, and thalamusF2.8%. Significant clusters of correlations of regional DA release with cognition and sensation-seeking behavior were observed. The current study demonstrates that [ 18 F]fallypride PET studies using oral D-AMPH (0.43 mg/kg) can be used to study D-AMPH-induced DA release in the striatal and extrastriatal regions in humans, and their relationship with cognition and sensation-seeking behavior.

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“…19 The B1 allele has also been shown to be associated with substance abuse. [6][7][8][9] Because of the importance of this question for the genetics of addiction, we measured both Taq1 20 The sampled population included 47 healthy controls and 23 subjects with schizophrenia. None of the subjects had a history of alcohol or substance abuse or dependence.…”

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D2 receptors binding potential is not affected by Taq1 polymorphism at the D2 receptor gene

1998

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Alcoholism and substance abuse have been associated with a polymorphism in a noncoding region of the D 2 receptor gene (the A1 allele of the Taq1 'A' system) in several, [1][2][3][4][5][6][7][8][9] but not all 10-13 studies. In addition, the presence of the A1 allele has been associated with lower density of D 2 receptors in the caudate nucleus in one postmortem study. 14 If the Taq1 'A1' allele is in linkage disequilibrium with a mutation that decreases the expression of the D 2 receptor gene, it is conceivable that subjects with the A1 allele might be predisposed to behaviors which stimulate dopamine transmission, such as alcoholism or substance abuse. In this study, we attempted to confirm the association between the A1 allele and lower D 2 receptor density, and explored a possible association between the B1 allele and D 2 receptor expression. Genotypes at the Taq1 'A' and 'B' systems were determined in 70 subjects who underwent in vivo measurement of D 2 receptors-binding potential with single photon emission computerized tomography (SPECT) and the selective dopamine D 2 receptor radiotracer [ 123 I]IBZM. [ 123 I]IBZM-binding potential was identical in A1 carriers (ie, subjects heterozygous or homozygous for that allele) (230 ± 85 ml g −1 , n = 27) and A1 noncarriers (231 ± 70 ml g −1 , n = 43). Similarly, we found no effect of the B1 allele on [ 123 I]IBZM-binding potential. In conclusion, the results of this study failed to replicate the previously reported association between A1 allele and lower D 2 receptor expression.In 1990, Blum et al 1 reported an association between alcoholism and a polymorphism in a noncoding region of the D 2 receptor gene (the A1 allele of the Taq1 'A' system). This association has been supported in several, 2-5 but not all subsequent studies. 10-13 The A1 allele was also found to be associated with prolonged P300 latency, reduced visuospatial preference, and low cerebral glucose utilization, all putative markers of alcoholism and dopamine function deficiency. [15][16][17] In addition, the A1 allele has also been associated with substance abuse, 6-9 which led to its conceptualization as a 'reward gene'. Together, these data suggest that this polymorphism might affect dopamine transmission in a way that predisposes subjects to 'reward seeking' behavior, i.e. behaviors aiming at increasing stimulation of dopamine transmission.The mechanism underlying the association between the A1 allele and vulnerability to addictive behaviors is unclear, since the Taq1 'A' polymorphism is not located in the coding region of the gene and a direct effect of this polymorphism on the structure of the D 2 receptor gene has been excluded by denaturing gradient gel electrophoresis mutational analysis study. 18 Noble et al 14 described an association between the A1 allele and decreased D 2 receptor density expressed in postmortem striatal samples from alcoholic and nonalcoholic subjects. If replicated, this observation might suggest that this polymorphism is in linkage disequilibrium with an unknown muta...

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Preparation and biodistribution of [125I]IBZM: A potential CNS D-2 dopamine receptor imaging agent

Cited by 75 publications

References 9 publications

Effects of Endogenous Neurotransmitters on the in vivo Binding of Dopamine and 5-HT Radiotracers in Mice

Effects of Endogenous Neurotransmitters on the in vivo Binding of Dopamine and 5-HT Radiotracers in Mice

Amphetamine-Induced Displacement of [18F] Fallypride in Striatum and Extrastriatal Regions in Humans

D2 receptors binding potential is not affected by Taq1 polymorphism at the D2 receptor gene

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