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

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Presentation on theme: "Carbon-11 epidepride: a suitable radioligand for PET investigation of striatal and extrastriatal dopamine D2 receptors  Oliver Langer, Christer Halldin,"— Presentation transcript:

1 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 (July 1999) DOI: /S (99)

2 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  , DOI: ( /S (99) )

3 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  , DOI: ( /S (99) )

4 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  , DOI: ( /S (99) )

5 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  , DOI: ( /S (99) )

6 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  , DOI: ( /S (99) )

7 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  , DOI: ( /S (99) )

8 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  , DOI: ( /S (99) )


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