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Showing content from https://link.springer.com/doi/10.1007/s002130050131 below:

Autoradiographic localisation of D3-dopamine receptors in the human brain using the selective D3-dopamine receptor agonist (+)-[3H]PD 128907

The selective D₃-dopamine receptor agonist 4aR,10bR-(+)-trans-3,4,4a,10b-tetrahydro-4-[N-propyl-2,3-³H]-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol ([³H]PD 128907) was used to visualise D₃-dopamine receptors in whole hemisphere cryosections from post-mortem human brain. [³H]PD 128907 has an 18- to 40-fold selectivity for D₃- over D₂-dopamine receptors as compared to a 7- to 24-fold selectivity of the more commonly used ligand [³H]7-OH-DPAT. [³H]PD 128907 accumulated markedly in the nucleus accumbens and in the ventral parts of caudate nucleus and putamen, with a slightly heterogeneous (patch-matrix like) distribution. The binding in the lateral parts of caudate nucleus and putamen was much less dense. No binding was obtained in any other regions. A very high proportion of [³H]PD 128907 was specifically bound, as judged from the low binding remaining in the presence of the D₂/D₃-dopamine receptor antagonist raclopride. This gives the ligand a potential for the detection of low density D₃-dopamine receptors in the human brain. The binding obtained with [³H]PD 128907 was qualitatively similar to that using [³H]7-OH-DPAT in the presence of GTP. However, [³H]7-OH-DPAT labelled, in contrast to [³H]PD 128907, also D₃-dopamine receptors in neocortex. The new compound [³H]PD 128907 appears to be a suitable radioligand for autoradiographic examination of the D₃-dopamine receptor localisation in the human brain, and should also be useful for pharmacological studies of this receptor subtype.

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1. Karolinska Institute, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, Stockholm, Sweden, , , , , , SE

   H. Hall, C. Halldin, Stefan Pauli, Lars Farde & Göran Sedvall

2. Department of Medicinal Chemistry, University of Groningen, Groningen, The Netherlands , , , , , , NL

   Durk Dijkstra & Håkan Wikström

3. Department of Psychiatric Disorders Chemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan, USA, , , , , , US

   Lawrence D. Wise

4. Department of Psychiatric Disorders Therapeutics, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan, USA, , , , , , US

   Thomas A. Pugsley

5. Unité de Neurobiologie et Pharmacologie, Centre Paul Broca de l’Inserm, 2ter Rue d’Alesia, Paris, France, , , , , , FR

   Pierre Sokoloff

1. H. Hall
2. C. Halldin
3. Durk Dijkstra
4. Håkan Wikström
5. Lawrence D. Wise
6. Thomas A. Pugsley
7. Pierre Sokoloff
8. Stefan Pauli
9. Lars Farde
10. Göran Sedvall

Received: 20 November 1995/Final version: 2 May 1996

Hall, H., Halldin, C., Dijkstra, D. et al. Autoradiographic localisation of D3-dopamine receptors in the human brain using the selective D3-dopamine receptor agonist (+)-[3H]PD 128907. Psychopharmacology 128, 240–247 (1996). https://doi.org/10.1007/s002130050131

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• Issue Date: December 1996

• DOI: https://doi.org/10.1007/s002130050131

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