Stereopsychopharmacology: Past, present and future

Smith, Donald F.

doi:10.1016/s0278-5846(84)80020-2

Progress in Neuro-Psychopharmacology and Biological Psychiatry

1984

DOI: 10.1016/s0278-5846(84)80020-2

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Stereopsychopharmacology: Past, present and future

Donald F. Smith¹

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1986

1990

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Cited by 7 publications

References 36 publications

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Stereoselective binding of 11C-raclopride in living human brain ? a search for extrastriatal central D2-dopamine receptors by PET

Farde

Pauli

Hall³

et al. 1988

Psychopharmacology

195

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The selective D2-dopamine receptor antagonist raclopride and its pharmacologically inactive (R)-enantiomer FLB472 were labelled with 11C and used in a study with positron emission tomography to examine the stereoselectivity of 11C-raclopride binding to central D2-dopamine receptors in three healthy men. After the injection of 11C-raclopride, there was a high accumulation of radioactivity in the dopamine-rich basal ganglia, whereas after the injection of 11C-FLB472 there was no such accumulation of radioactivity. Thus, the binding of 11C-raclopride is stereoselective. Distribution ratios [radioactivity in a brain region/"free" (not protein-bound) radioactivity in plasma] were calculated for the two enantiomers to study regional differences in the accumulation of radioactivity. The distribution ratios in white matter were similar for the two enantiomers. In the putamen, a three to four-fold higher distribution ratio was found for 11C-raclopride than for 11C-FLB472, reflecting the presence of specific binding of 11C-raclopride binding to D2-dopamine receptors in the basal ganglia. In the temporal and frontal cortices the distribution ratios were, however, only a few per cent higher for 11C-raclopride than for 11C-FLB472, indicating that if D2-dopamine receptors are present in the human neocortex, then their density is indeed very low.

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Stereoselective binding of 11C-raclopride in living human brain ? a search for extrastriatal central D2-dopamine receptors by PET

Farde

Pauli

Hall³

et al. 1988

Psychopharmacology

195

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Antinociceptive effects of the stereoisomers of nicotine given intrathecally in spinal rats

Christensen

Smith

1990

J. Neural Transmission

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Spinalized rats received an intrathecal injection of either (-)-nicotine or (+)-nicotine in order to study the stereoselectivity of antinociception. Pain threshold was measured using the tail-flick test. Both stereoisomers had anti-nociceptive effects, but (-)-nicotine was up to 970 times more potent, depending on test conditions. The antinociceptive action of (-)-nicotine was antagonized by mecamylamine and yohimbine but not by naloxone and atropine. The findings show that spinal mechanisms are highly stereoselective toward nicotine, and suggest that primarily nicotinergic and alpha-adrenergic receptors are involved in its central antinociceptive effects.

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The stereoselectivity of serotonin uptake in brain tissue and blood platelets: The topography of the serotonin uptake area

Smith¹

1986

Neuroscience & Biobehavioral Reviews

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Stereopsychopharmacology: Past, present and future

Cited by 7 publications

References 36 publications

Stereoselective binding of 11C-raclopride in living human brain ? a search for extrastriatal central D2-dopamine receptors by PET

Stereoselective binding of 11C-raclopride in living human brain ? a search for extrastriatal central D2-dopamine receptors by PET

Antinociceptive effects of the stereoisomers of nicotine given intrathecally in spinal rats

The stereoselectivity of serotonin uptake in brain tissue and blood platelets: The topography of the serotonin uptake area

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