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  • Title: Dopamine receptors labelled by [3H]quinpirole.
    Author: Seeman P, Schaus JM.
    Journal: Eur J Pharmacol; 1991 Oct 02; 203(1):105-9. PubMed ID: 1686763.
    Abstract:
    Since quinpirole (or LY171555) has a high affinity for dopamine D2 receptors, and since the high-affinity state of D2 appears to be the functional state of D2, we prepared [3H]quinpirole to investigate its suitability for labelling the high-affinity state of the D2 receptor. The dissociation constant of [3H]quinpirole binding to canine striatum homogenate was 3.9 nM in the absence of NaCl and 6.8 nM in the presence of NaCl. Only 50% of the total binding was specifically displaced by 10 microM S-sulpiride. The data are consistent with the conclusion that much or most of the [3H]quinpirole binds to the high-affinity state of the D2 receptor, since dopamine D2 agonists and antagonists were the most potent in inhibiting the binding of this ligand, because the density of binding sites was 8-9 pmol/g, about half that for [3H]spiperone, and because the density was reduced by 70% in the presence of guanylylimidodiphosphate. Since quinpirole has a reported Ki value of 5.1 nM for dopamine D3 receptors, similar to the quinpirole Ki value of 4.8 nM for the high-affinity state of the dopamine D2 receptor, it appears that [3H]quinpirole with its Kd of 3.9-6.8 nM could label both these two dopamine receptors. However, since the spiperone and haloperidol Ki values against [3H]quinpirole were the same as their values at dopamine D2 receptors rather than dopamine D3 receptors, it appears that [3H]quinpirole predominantly labels dopamine D2 receptors in the canine striatum. The guanine nucleotide-insensitive component of [3H]quinpirole binding (about 30%) may be to dopamine D3 receptors.
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