ISSN:
1432-2072
Keywords:
[123I]β-CIT
;
Dopamine transporter
;
Cocaine
;
Medication development
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract The in vivo potency of euphorigenic doses of intravenous cocaine for displacing [123I]β-CIT ([123I]2β-carbomethoxy-3β-(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]β-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 (P〈0.0005) 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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02246266
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