Details

Autor(en) / Beteiligte

• Aquilonius, S.-M.
• Bertröm, K.
• Eckernäs, S-Å.
• Hartvig, P.
• Leenders, K.L.
• Lundquist, H.
• Antoni, G.
• Gee, A.
• Rimland, A.
• Uhlin, J.
• Långström, B.

Titel

In vivo evaluation of striatal dopamine reuptake sites using 11C-nomifensine and positron emission tomography

Ist Teil von

• Acta neurologica Scandinavica, 1987-10, Vol.76 (4), p.283-287

Ort / Verlag

Oxford, UK: Blackwell Publishing Ltd

Erscheinungsjahr

1987

Quelle

MEDLINE

Beschreibungen/Notizen

• In vitro nomifensine demonstrates high affinity and specificity for dopamine reuptake sites in the brain. In the present study 11C‐nomifensine was administered i.v. in trace amounts (10–50μg) to ketamine anaesthetized Rhesus monkeys (6–10 kg b.w.) and the time‐course of radioactivity within different brain regions was measured by positron emission tomography (PET). Six base‐line experiments lasting for 60–80 min were performed. The procedure was repeated after pretreatment with nomifensine (2–6 mg/kg i.v.), another reuptake inhibitor, mazindol (0,3 mg/kg i.v.), desipramine (0.5 mg/kg i.v) or spiperone (0.3 mg/kg i.v.) before the administration of a second 11C‐nomifensine dose. The highest radioactivity uptake was found in the dopamine innervated striatum and the lowest in a region containing the cerebellum, known to be almost devoid of dopaminergic neurons. The difference between striatal and cerebellar uptake of 11C‐nomifensine derived radioactivity was markedly reduced after nomifensine and mazindol but not after desipramine and spiperone. These results indicate that in vivo the striatal uptake of 11C‐nomifensine, as measured with PET, involves specific binding with the dopamine reuptake sites. In the first human applications of 11C‐nomifensine and PET in a healthy volunteer, the regional uptake of radioactivity was similar to that in base‐line experiments with Rhesus monkeys. In the healthy subject the striatal/cerebellar ratio was 1.6, 50 min after the injection of 11C‐nomifensine. In a hemi‐parkinsonian patient this ratio was 1.1 contralaterally and 1.3 ipsilaterally to the affected side. 11C‐nomifensine and PET seems to be an auspicious method to measure the striatal dopaminergic nerve terminals of man in vivo.