Euphorigenic doses of cocaine reduce [123I]β-CIT SPECT measures of dopamine transporter availability in human cocaine addicts
| Autor: | Thomas R. Kosten, E. A. Wallace, Robert T. Malison, S. E. Best, Marc Laruelle, J. S. Seibyl, Sami S. Zoghbi, Robert B. Innis, Lawrence H. Price, Elinore McCance, Paul B. Hoffer, Ronald M. Baldwin |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
Substance-Related Disorders
Nerve Tissue Proteins Pharmacology chemistry.chemical_compound Cocaine Dopamine Uptake Inhibitors In vivo Dopamine medicine Humans Potency ED50 Dopamine transporter Tomography Emission-Computed Single-Photon Dopamine Plasma Membrane Transport Proteins Membrane Glycoproteins biology Chemistry Membrane Transport Proteins Binding potential Tropane biology.protein Catecholamine Carrier Proteins medicine.drug |
| Zdroj: | Psychopharmacology. 122:358-362 |
| ISSN: | 1432-2072 0033-3158 |
| Popis: | The in vivo potency of euphorigenic doses of intravenous cocaine for displacing [123I]beta-CIT ([123I]2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane) binding to striatal dopamine transporters (DAT) was assessed in human cocaine addicts using single photon emission computed tomography (SPECT). Cocaine-dependent subjects (n = 6) were injected with [123I]beta-CIT and imaged 24 h later under equilibrium conditions. Sequential cocaine infusions (0.28 +/- 0.03 and 0.56 +/- 0.07 mg/kg) produced significant (P0.0005) reductions in the specific to non-specific equilibrium partition coefficient, V3" (6 +/- 6 and 17 +/- 3%), a measure proportional to DAT binding potential. Regression analysis of the logit transformed data enabled reliable determination of the Hill coefficient (0.51) and 50% displacement (ED50) dose of cocaine (2.8 mg/kg). These preliminary data suggest that cocaine produces behavioral effects in humans at measurable levels of DAT occupancy. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink