title: Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist.
abstract: A series of microPET imaging studies were conducted in anesthetized rhesus monkeys using the dopamine D2-selective partial agonist, [(11)C]SV-III-130. There was a high uptake in regions of brain known to express a high density of D2 receptors under baseline conditions. Rapid displacement in the caudate and putamen, but not in the cerebellum, was observed after injection of the dopamine D2/3 receptor nonselective ligand S(-)-eticlopride at a low dosage (0.025mg/kg/i.v.); no obvious displacement in the caudate, putamen and cerebellum was observed after the treatment with a dopamine D3 receptor selective ligand WC-34 (0.1mg/kg/i.v.). Pretreatment with lorazepam (1mg/kg, i.v. 30min) to reduce endogenous dopamine prior to tracer injection resulted in unchanged binding potential (BP) values, a measure of D2 receptor binding in vivo, in the caudate and putamen. d-Amphetamine challenge studies indicate that there is a significant displacement of [(11)C]SV-III-130 by d-Amphetamine-induced increases in synaptic dopamine levels.
authors: Department of Radiology, Washington University School of Medicine, 510 S. Kingshighway Blvd., St. Louis, MO 63110, USA.
authors: Jinbin
authors: J
authors: Xu
authors: Suwanna
authors: S
authors: Vangveravong
authors: Shihong
authors: S
authors: Li
authors: Jinda
authors: J
authors: Fan
authors: Lynne A
authors: LA
authors: Jones
authors: Jinquan
authors: J
authors: Cui
authors: Ruike
authors: R
authors: Wang
authors: Zhude
authors: Z
authors: Tu
authors: Wenhua
authors: W
authors: Chu
authors: Joel S
authors: JS
authors: Perlmutter
authors: Robert H
authors: RH
authors: Mach
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics*; D018491:Dopamine Agonists / Q000493:pharmacokinetics; D008253:Macaca mulatta; D008297:Male; D010879:Piperazines / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods*; D015363:Quinolones / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D017448:Receptors, Dopamine D2 / Q000819:agonists*
chemical_list: C561104:7-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one; D002250:Carbon Radioisotopes; D018491:Dopamine Agonists; D010879:Piperazines; D015363:Quinolones; D019275:Radiopharmaceuticals; D017448:Receptors, Dopamine D2