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- W2053307595 abstract "In search of a potent and selective radioiodinated ligand for the 5-hydroxytryptamine (serotonin or 5-HT) uptake complex, we synthesized and evaluated the in vitro properties of [125I]5-iodo-6-nitroquipazine. The binding properties and pharmacological profile of this radioligand were studied in rat brain homogenates, and it was found to display high affinity and selectivity for the serotonin uptake complex. Scatchard analysis of the binding data indicated a single population of sites with aKd of23 ± 6pM and aBmax of 430 ± 50 fmol/mg protein (mean ±S.E.M., n - 7). Inhibitors of serotonin uptake were the most efficient competitors for [125I]5-iodo-6-nitroquipazine binding withKi values similar in rank order and magnitude to those obtained in studies of other established serotonin uptake blockers. Inhibitors of dopamine and norepinephrine uptake as well as a wide variety of postsynaptic receptor agents were relatively ineefective in inhibiting [125I]5-iodo-6-nitroquipazine binding to rat brain membranes. Serotonin was the only monoaminergic neurotransmitter capable of effectively competing for [125I]5-iodo-6-nitroquipazine binding sites and gave aKi value of 2.8 ± 0.6 μM. Lesions of the serotonergic system withp-chloroamphetamine resulted in a dramatic loss 90%of [125I]5-iodo-6-nitroquipazine binding to rat cortical membranes. Non-radiolabeled 5-iodo-6-nitroquipazine potently inhibited the binding of [3H]paroxetine to serotonin reuptake sites in rat cortical membranes with aKi of 0.17 ± 0.06nM. These results demonstrate that 5-iodo-6-nitroquipazine is a potent and selective ligand for the serotonin uptake complex, and the [125I]-labeled radioligand has an advantage of detecting low levels of binding sites." @default.
- W2053307595 created "2016-06-24" @default.
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- W2053307595 date "1993-08-01" @default.
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- W2053307595 title "[125I]5-iodo-6-nitroquipazine: a potent and selective ligand for the 5-hyfroxytryptamine uptake complex. I. In vitro studies" @default.
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- W2053307595 doi "https://doi.org/10.1016/0006-8993(93)91616-z" @default.
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