Carbon-11 epidepride: a suitable radioligand for PET investigation of striatal and extrastriatal dopamine D2 receptors Oliver Langer, Christer Halldin,

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Carbon-11 epidepride: a suitable radioligand for PET investigation of striatal and extrastriatal dopamine D2 receptors Oliver Langer, Christer Halldin, Frédéric Dollé, Carl-Gunnar Swahn, Hans Olsson, Per KarlssonHåkan HallJohan SandellCamilla Lundkvist, Franzoise Vaufrey, Christian Loc’h, Christian Crouzel, Bernard Mazière, Lars Farde Nuclear Medicine and Biology Volume 26, Issue 5, Pages 509-518 (July 1999) DOI: 10.1016/S0969-8051(99)00005-0

FIG. 1 Synthesis of the desmethyl-precursor 5 via two different synthetic pathways and carbon-11 labeling with [11C]methyl triflate to obtain [11C]epidepride. Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)

FIG. 2 Semipreparative high performance liquid chromatography (HPLC) chromatograms (ultraviolet and radioactivity vs. time) using a normal phase Waters μ-Porasil column. Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)

FIG. 3 Autoradiogram showing human postmortem whole-hemisphere autoradiography using [11C]epidepride. Top: control; bottom: inhibition with raclopride (10 μM). (Note: Fig. 4 is located on page 514) Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)

FIG. 4 Time course of brain radioactivity (nCi/mL) in a cynomolgus monkey. (A) Regional brain radioactivity after intravenous administration of [11C]epidepride. (B) Pretreatment with raclopride (1 mg/kg, 33 min before injection). (C) Specific binding in the striatum, neocortex, and thalamus. (D) Specific binding ratio. The positron emission tomography (PET)-camera system was a Siemens ECAT EXACT HR. Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)

FIG. 5 Colour-coded positron emission tomography (PET) image showing the distribution of radioactivity in a cynomolgus monkey brain after intravenous administration of [11C]epidepride (measured from 9 to 90 min). Control (left) and pretreatment with raclopride (1 mg/kg, 33 min before injection) (right). The PET-camera system was a Siemens ECAT EXACT HR. Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)

FIG. 6 A reversed-phase high performance liquid chromatography (HPLC) chromatogram of a cynomolgus monkey plasma sample obtained 16 min after intravenous administration of [11C]epidepride. Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)

FIG. 7 Percentage of unchanged [11C]epidepride in monkey plasma versus time (left) and total radioactivity in plasma and radioactivity from unchanged parent compound (nCi/mL) (right). Nuclear Medicine and Biology 1999 26, 509-518DOI: (10.1016/S0969-8051(99)00005-0)