Mapping cocaine binding sites in human and baboon brain in vivo

J. S. Fowler, N. D. Volkow, A. P. Wolf, S. L. Dewey, D. J. Schlyer, R. R. MacGregor, Robert Hitzemann, J. Logan, B. Bendriem, S. J. Gatley, D. Christman

Research output: Contribution to journalArticle

270 Citations (Scopus)

Abstract

The first direct measurements of cocaine binding in the brain of normal human volunteers and baboons have been made by using positron emission tomography (PET) and tracer doses of [N-11C-methyl]-(-)-cocaine ([11C]cocaine). Cocaine's binding and release from brain are rapid with the highest regional uptake of carbon-11 occurring in the corpus striatum at 4-10 minutes after intravenous injection of labeled cocaine. This was followed by a clearance to half the peak value at about 25 minutes with the overall time course paralleling the previously documented time course of the euphoria experienced after intravenous cocaine administration. Blockade of the dopamine reuptake sites with nomifensine reduced the striatal but not the cerebellar uptake of [11C]cocaine in baboons indicating that cocaine binding is associated with the dopamine reuptake site in the corpus striatum. A comparison of labeled metabolites of cocaine in human and baboon plasma showed that while cocaine is rapidly metabolized in both species, the profile of labeled metabolites is different, with baboon plasma containing significant amounts of labeled carbon dioxide, and human plasma containing no significant labeled carbon dioxide. These studies demonstrate the fesibility of using [11C]cocaine and PET to map binding sites for cocaine in human brain, to monitor its kinetics, and to characterize its binding mechanism by using appropriate pharmacological challenges

Original languageEnglish (US)
Pages (from-to)371-377
Number of pages7
JournalSynapse
Volume4
Issue number4
DOIs
StatePublished - 1989
Externally publishedYes

Fingerprint

Papio
Cocaine
Binding Sites
Brain
Corpus Striatum
Carbon Dioxide
Positron-Emission Tomography
Dopamine
Nomifensine
Intravenous Injections
Intravenous Administration
Healthy Volunteers
Carbon
Pharmacology

ASJC Scopus subject areas

  • Neuroscience(all)
  • Physiology
  • Pharmacology

Cite this

Fowler, J. S., Volkow, N. D., Wolf, A. P., Dewey, S. L., Schlyer, D. J., MacGregor, R. R., ... Christman, D. (1989). Mapping cocaine binding sites in human and baboon brain in vivo. Synapse, 4(4), 371-377. https://doi.org/10.1002/syn.890040412

Mapping cocaine binding sites in human and baboon brain in vivo. / Fowler, J. S.; Volkow, N. D.; Wolf, A. P.; Dewey, S. L.; Schlyer, D. J.; MacGregor, R. R.; Hitzemann, Robert; Logan, J.; Bendriem, B.; Gatley, S. J.; Christman, D.

In: Synapse, Vol. 4, No. 4, 1989, p. 371-377.

Research output: Contribution to journalArticle

Fowler, JS, Volkow, ND, Wolf, AP, Dewey, SL, Schlyer, DJ, MacGregor, RR, Hitzemann, R, Logan, J, Bendriem, B, Gatley, SJ & Christman, D 1989, 'Mapping cocaine binding sites in human and baboon brain in vivo', Synapse, vol. 4, no. 4, pp. 371-377. https://doi.org/10.1002/syn.890040412
Fowler JS, Volkow ND, Wolf AP, Dewey SL, Schlyer DJ, MacGregor RR et al. Mapping cocaine binding sites in human and baboon brain in vivo. Synapse. 1989;4(4):371-377. https://doi.org/10.1002/syn.890040412
Fowler, J. S. ; Volkow, N. D. ; Wolf, A. P. ; Dewey, S. L. ; Schlyer, D. J. ; MacGregor, R. R. ; Hitzemann, Robert ; Logan, J. ; Bendriem, B. ; Gatley, S. J. ; Christman, D. / Mapping cocaine binding sites in human and baboon brain in vivo. In: Synapse. 1989 ; Vol. 4, No. 4. pp. 371-377.
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