HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

beta-CIT SPECT demonstrates blockade of 5HT-uptake sites by citalopram in the human brain in vivo.

Abstract
The cocaine analogue 2-beta-carbomethoxy-3-beta-(4-iodophenyl)-tropane (beta-CIT) is a potent ligand for both dopamine- and serotonin uptake sites which in its 123I labeled form can be used for single photon emission computerized tomography (SPECT). It was demonstrated previously by SPECT-studies in non-human primates that 123I-beta-CIT binds to dopamine transporters in the striatum and to serotonin transporters in hypothalamus and midbrain. The aim of the present study was to compare 123I-beta-CIT binding in the brain stem of normal controls and a group of subjects under treatment with the selective serotonin reuptake inhibitor (SSRI) citalopram. 123I-beta-CIT-SPECT was performed in 12 depressed patients under 20 mg (n = 5), 40 mg (n = 6) and 60 mg (n = 1) citalopram daily, in one untreated depressed patient and in 11 controls at regular time intervals up till 24 hours p.inj. A highly significant reduction of beta-CIT binding was found in an area including mesial thalamus, hypothalamus, midbrain and pons in patients under citalopram compared to controls (44.1 +/- 14.4 vs. 82.3 +/- 18.6cpm's/mCi x kg body weight; specific binding 4 hrs p.inj.; p = 0.0001). No differences were seen between the high and low dose group and no changes were found in the striatum. 123I-beta-CIT binding in the brain stem and striatum in one untreated depressed patient fell within the range of control values. To our knowledge this is the first report directly demonstrating the effect of a selective serotonin uptake inhibitor in the brain in humans in vivo. SPECT measurements of serotonin uptake sites in patients with depression and other psychiatric disorders might provide better insights into the pathophysiology of these disorders and into mechanisms of drug action.
AuthorsW Pirker, S Asenbaum, S Kasper, H Walter, P Angelberger, G Koch, A Pozzera, L Deecke, I Podreka, T Brücke
JournalJournal of neural transmission. General section (J Neural Transm Gen Sect) Vol. 100 Issue 3 Pg. 247-56 ( 1995) Austria
PMID8748670 (Publication Type: Journal Article)
Chemical References
  • Iodine Radioisotopes
  • Ligands
  • Serotonin Uptake Inhibitors
  • Citalopram
  • Serotonin
  • 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
  • Cocaine
Topics
  • Adult
  • Aged
  • Brain Chemistry (drug effects)
  • Brain Stem (drug effects)
  • Citalopram (pharmacology)
  • Cocaine (analogs & derivatives, pharmacology)
  • Female
  • Humans
  • Hypothalamus (drug effects)
  • Iodine Radioisotopes
  • Ligands
  • Male
  • Middle Aged
  • Neostriatum (drug effects)
  • Serotonin (metabolism)
  • Selective Serotonin Reuptake Inhibitors (pharmacology)
  • Tomography, Emission-Computed, Single-Photon

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: