Kinetics of the uptake of [3H]paroxetine in the rat brain.
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Kinetics of the uptake of [3H]paroxetine in the rat brain. / Cumming, P; Gjedde, A.
In: Synapse, Vol. 15, No. 2, 1993, p. 124-9.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Kinetics of the uptake of [3H]paroxetine in the rat brain.
AU - Cumming, P
AU - Gjedde, A
PY - 1993
Y1 - 1993
N2 - Paroxetine, an antidepressant with a high affinity for serotonin (5-HT) re-uptake sites, is a potential tracer of these sites. We determined the kinetic properties of [3H]paroxetine in rat brain in vivo. Relative to [14C]iodo-antipyrine, the brain uptake index (BUI) of [3H]paroxetine was 60-70%. The unidirectional blood clearance of [3H]paroxetine were 0.05-0.12 ml g-1 min-1, lower than expected from the BUI values. The steady state volume of distribution was 3.5 ml hg-1 in the diencephalon and 1.8 ml g-1 in the cerebellum, suggesting a binding potential of unity. Autoradiographs at four hours after [3H]paroxetine injection (300 microCi, i.p.) revealed heterogeneous binding consistent with the calculated binding potentials. Binding was nearly absent from cerebellum and was highest in the dorsal raphe, superior colliculus, dorsal hypothalamus, and entorhinal cortex, but did not reach equilibrium in four hours of tracer circulation. The specific binding relative to vermis was displaced by pretreatment with fluoxetine (10 mg/kg, i.p.).
AB - Paroxetine, an antidepressant with a high affinity for serotonin (5-HT) re-uptake sites, is a potential tracer of these sites. We determined the kinetic properties of [3H]paroxetine in rat brain in vivo. Relative to [14C]iodo-antipyrine, the brain uptake index (BUI) of [3H]paroxetine was 60-70%. The unidirectional blood clearance of [3H]paroxetine were 0.05-0.12 ml g-1 min-1, lower than expected from the BUI values. The steady state volume of distribution was 3.5 ml hg-1 in the diencephalon and 1.8 ml g-1 in the cerebellum, suggesting a binding potential of unity. Autoradiographs at four hours after [3H]paroxetine injection (300 microCi, i.p.) revealed heterogeneous binding consistent with the calculated binding potentials. Binding was nearly absent from cerebellum and was highest in the dorsal raphe, superior colliculus, dorsal hypothalamus, and entorhinal cortex, but did not reach equilibrium in four hours of tracer circulation. The specific binding relative to vermis was displaced by pretreatment with fluoxetine (10 mg/kg, i.p.).
U2 - 10.1002/syn.890150204
DO - 10.1002/syn.890150204
M3 - Journal article
C2 - 8259523
VL - 15
SP - 124
EP - 129
JO - Synapse
JF - Synapse
SN - 0887-4476
IS - 2
ER -
ID: 14945549