Positron emission tomographic evaluation of the putative dopamine-D3 receptor ligand, [11C]RGH-1756 in the monkey brain

Neurochemistry International
Judit SóvágóBalázs Gulyás

Abstract

The dopamine-D3 receptor is of special interest due to its postulated role in the pathophysiology and treatment of schizophrenia and Parkinson's Disease. Increasing evidences support the assumption that the D3 receptors are occupied to a high degree by dopamine at physiological conditions. Research on the functional role of the D3 receptors in brain has however been hampered by the lack of D3 selective ligands. In the present Positron Emission Tomography (PET) study the binding of the novel, putative dopamine-D3 receptor ligand, [11C]RGH-1756 was characterized in the cynomolgus monkey brain. [11C]RGH-1756 was rather homogenously distributed in brain and the regional binding potential (BP) values ranged between 0.17 and 0.48. Pretreatment with unlabelled RGH-1756 decreased radioligand binding to the level of the cerebellum in most brain areas. The regional BP values were lower after intravenous injection of a higher mass of RGH-1756, indicating saturable binding of [11C]RGH-1756. The D2/D3 antagonist raclopride partly inhibited the binding of [11C]RGH-1756 in several brain areas, including the striatum, mesencephalon and neocortex, whereas the 5HT(1A) antagonist WAY-100635 had no evident effect on [11C]RGH-1756 binding. Despite ...Continue Reading

Citations

May 10, 2005·Nuclear Medicine and Biology·Sjoerd J FinnemaChrister Halldin
Sep 16, 2009·The International Journal of Neuropsychopharmacology·Ariel Graff-GuerreroShitij Kapur
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Olaf PranteAshutosh Banerjee
Sep 15, 2007·Neuroscience and Biobehavioral Reviews·Szabolcs Kéri
May 27, 2005·Journal of Medicinal Chemistry·Amy Hauck NewmanMichael A Nader

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