Quantitative autoradiography of cocaine binding sites in human brain postmortem

A. Biegon, K. Dillon, N. D. Volkow, Robert Hitzemann, J. S. Fowler, A. P. Wolf

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

Quantitative autoradiography was used to study cocaine binding sites in the human brain postmortem. Tritiated cocaine was applied to brain sections from three drug- and disease-free subjects at a low (10 nM) concentration and at a high (1 μM) concentration, the latter being in the range of brain concentrations of cocaine found in users of the drug. Nonspecific binding was assessed in the presence of 100 μM unlabeled cocaine. At low (10 nM) concentrations of labeled cocaine, the basal ganglia exhibit the highest density of binding sites, with considerably lower densities in thalamus, cortex, and hippocampus. Cocaine binding at high (1 μM) concentrations displayed a different distribution pattern, more homogeneous with some cortical regions exhibiting binding site densities close to those seen in the basal ganglia. Preliminary competition experiments with several drugs indicate that dopamine uptake inhibitors completely block cocaine binding to the basal ganglia, while serotonin uptake inhibitors were more effective in the hippocampus. These findings suggest that cocaine binds to dopamine uptake sites in the human basal ganglia postmortem but that it also interacts with other classes of binding sites, depending on the concentration and brain region examined.

Original languageEnglish (US)
Pages (from-to)126-130
Number of pages5
JournalSynapse
Volume10
Issue number2
StatePublished - 1992
Externally publishedYes

Fingerprint

Autoradiography
Cocaine
Binding Sites
Brain
Basal Ganglia
Hippocampus
Dopamine Uptake Inhibitors
Serotonin Uptake Inhibitors
Drug Users
Thalamus
Pharmaceutical Preparations
Dopamine

ASJC Scopus subject areas

  • Physiology
  • Neuroscience(all)
  • Pharmacology

Cite this

Biegon, A., Dillon, K., Volkow, N. D., Hitzemann, R., Fowler, J. S., & Wolf, A. P. (1992). Quantitative autoradiography of cocaine binding sites in human brain postmortem. Synapse, 10(2), 126-130.

Quantitative autoradiography of cocaine binding sites in human brain postmortem. / Biegon, A.; Dillon, K.; Volkow, N. D.; Hitzemann, Robert; Fowler, J. S.; Wolf, A. P.

In: Synapse, Vol. 10, No. 2, 1992, p. 126-130.

Research output: Contribution to journalArticle

Biegon, A, Dillon, K, Volkow, ND, Hitzemann, R, Fowler, JS & Wolf, AP 1992, 'Quantitative autoradiography of cocaine binding sites in human brain postmortem', Synapse, vol. 10, no. 2, pp. 126-130.
Biegon A, Dillon K, Volkow ND, Hitzemann R, Fowler JS, Wolf AP. Quantitative autoradiography of cocaine binding sites in human brain postmortem. Synapse. 1992;10(2):126-130.
Biegon, A. ; Dillon, K. ; Volkow, N. D. ; Hitzemann, Robert ; Fowler, J. S. ; Wolf, A. P. / Quantitative autoradiography of cocaine binding sites in human brain postmortem. In: Synapse. 1992 ; Vol. 10, No. 2. pp. 126-130.
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