The effects of kainic acid and 6-hydroxydopamine lesions, metal ions and GTP on in vitro binding of the D-2 dopamine agonist, [3H]N-0437, to striatal membranes

Weide, Jan van der; Vries, J. B. De; Tepper, Pieter G.; Horn, Alan S.

doi:10.1016/0014-2999(87)90739-4

Cited by 16 publications

(1 citation statement)

References 24 publications

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“…; n --i each) had little effect on the dopamine D~ binding measured by [z~C]SCH23390, the k3 value for the dopamine D2 receptor and the uptake ratio of dopamine D3 receptor were significantly decreased by R-THBP. These results are consistent with the results from an in vitro study ) that showed that R-THBP selectively affected the binding of [3H]N-0437, which ligand is selective for pre-and postsynaptic dopamine D 2 receptors (Van der Weide et al, 1987Weide et al, , 1988, but had no effect on [3H]SCH23390 binding to the striatal membrane fraction. A microdialysis study using rats has shown that the endogenous level of R-THBP regulates dopamine release, since R-THBP has a dopaminereleasing action independent of its role in the biosynthesis of' dopamine and since dopamine output from the striatum was markedly decreased by multiple administration of 2,4-diamino-6-hydroxypyrimidine (DAHP), an inhibitor of the rate-limiting enzyme for R-THBP biosynthesis (Mataga et al, 1990;Tani et al, 1992).…”

Section: Pharmacodynamics Of R-thbpsupporting

confidence: 94%

Effects of 6R-L-erythro-5,6,7,8-tetrahydrobiopterin on the dopaminergic and cholinergic receptors as evaluated by positron emission tomography in the Rhesus monkey

Tani

Ishihara

Kanai

et al. 1995

J. Neural Transmission

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The effects of 6R-L-erythro-5,6,7,8-tetrahydrobiopterin (R-THBP) on the central cholinergic and dopaminergic systems in the Rhesus monkey brain were investigated by positron emission tomography (PET) with the muscarinic cholinergic receptor ligands (N-[11C]methyl-benztropine) and dopaminergic receptor ligands selective for D1, D2, and D3 subtypes ([11C]SCH23390, N-[11C]methyl-spiperone, and (+)[11C]UH232, respectively). None of the doses (3, 10, and 30 mg/kg i.v.) of R-THBP used significantly affected the regional cerebral blood flow (rCBF as determined by Raichle's H(2)15O method), and 10 mg/kg of R-THBP had little effect on the regional cerebral metabolic rate of glucose (rCMRglc) in the Rhesus monkey brain, as assessed by the graphical [18F]fluoro-deoxyglucose method. The effect of R-THBP on the muscarinic cholinergic system was dose dependent; while 3 mg/kg of R-THBP did not significantly alter the uptake ratio of N-[11C]methylbenztropine in several brain regions to that in the cerebellum, 10 and 30 mg/kg of R-THBP significantly reduced the uptake ratio in the thalamus, as well as in the frontal and temporal cortices. None of the doses (3, 10, and 30 mg/kg i.v.) of R-THBP tested affected [11C]SCH23390 (dopamine D1 receptor) binding. However, the k3 value for N-[11C]methyl-spiperone (dopamine D2 receptor) binding, which represents the association rate X Bmax value, was significantly decreased in the striatum. The uptake ratio of (+)[11C]UH232 (dopamine D3 receptor) in the striatum to that in the cerebellum was also decreased by administration of R-THBP (3 and 30 mg/kg i.v.). These findings suggest that R-THBP acts on dopamine D2 and D3 receptors selectively without markedly affecting dopamine D1 receptor binding. Furthermore, the changes in cholinergic and dopamine D2 and D3 receptors in vivo can not be attributed to a change in rCBF but may depend on the action of R-THBP.

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Section: Pharmacodynamics Of R-thbpsupporting

confidence: 94%

Effects of 6R-L-erythro-5,6,7,8-tetrahydrobiopterin on the dopaminergic and cholinergic receptors as evaluated by positron emission tomography in the Rhesus monkey

Tani

Ishihara

Kanai

et al. 1995

J. Neural Transmission

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6-Hydroxydopamine-Induced Lesions of Dopaminergic Neurons Alter the Function of Postsynaptic Cholinergic Neurons without Changing Cytoskeletal Proteins

Muma

Lee

Gorman³

et al. 2001

Experimental Neurology

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Search for PET probes for imaging the globus pallidus studied with rat brainex vivo autoradiography

et al. 2000

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We have evaluated the feasibility of using four positron emission tomography (PET) tracers for imaging the globus pallidus by ex vivo autoradiography in rats. The tracers investigated were [11C]KF18446, [11C]SCH 23390 and [11C]raclopride for mapping adenosine A2A, dopamine D1 and dopamine D2 receptors, respectively, and [18F]FDG. The highest uptake by the globus pallidus was found for [11C]SCH 23390, followed by [18F]FDG, [11C]KF18446 and [11C]raclopride. The receptor-specific uptake by the globus pallidus was observed in [11C]KF18446 and [11C]SCH 23390, but not in [11C]raclopride. Uptake ratios of globus pallidus to the striatum for [18F]FDG and [11C]KF18446 were approximately 0.6, which was twice as large as that for [11C]SCH 23390. In a rat model of degeneration of striatopallidal gamma-aminobutyric acid-ergic-enkephalin neurons induced by intrastriatal injection of quinolinic acid, the uptake of [11C]KF18446 by the striatum and globus pallidus was remarkably reduced. To prove the visualization of the globus pallidus by PET with [18F]FDG and [11C]KF18446, PET-MRI registration technique and advances in PET technologies providing high-resolution PET scanner will be required. The metabolic activity of the globus pallidus could then be measured by PET with [18F]FDG, and [11C]KF18446 may be a candidate tracer for imaging the pallidal terminals projecting from the striatum.

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The effects of kainic acid and 6-hydroxydopamine lesions, metal ions and GTP on in vitro binding of the D-2 dopamine agonist, [3H]N-0437, to striatal membranes

Cited by 16 publications

References 24 publications

Effects of 6R-L-erythro-5,6,7,8-tetrahydrobiopterin on the dopaminergic and cholinergic receptors as evaluated by positron emission tomography in the Rhesus monkey

Effects of 6R-L-erythro-5,6,7,8-tetrahydrobiopterin on the dopaminergic and cholinergic receptors as evaluated by positron emission tomography in the Rhesus monkey

6-Hydroxydopamine-Induced Lesions of Dopaminergic Neurons Alter the Function of Postsynaptic Cholinergic Neurons without Changing Cytoskeletal Proteins

Search for PET probes for imaging the globus pallidus studied with rat brainex vivo autoradiography

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