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- W2012808016 abstract "In order to fully resolve the binding profile of [3H]rauwolscine to membranes from the cortex of the rat, saturation, competition and association-dissociation data were analysed by means of computerised curve-fitting techniques. The binding isotherm for [3H]rauwolscine was best fitted to a two-component model consisting of a high-affinity, saturable site (approx. Kd 1.8 nM) and a low-affinity, apparently non-saturable, component. Displacement experiments revealed shallow inhibition curves for both antagonist and agonist ligands with a rank order of potency indicative of an interaction at the alpha 2-adrenoceptor. Inclusion of spiroperidol, but not prazosin, markedly steepened the antagonist, but not the agonist inhibition curves. In addition, spiroperidol attenuated, but did not eliminate, the low-affinity component in saturation experiments. Dissociation and association data revealed a biphasic paradigm, the more slowly-associating/dissociating component of which was sensitive to spiroperidol. It was concluded that [3H]rauwolscine binds to two sites on membranes of the rat cortex; a high-affinity site corresponding to alpha 2-adrenoceptors and a low-affinity, spiroperidol-sensitive component. The possible identity of the low-affinity site is discussed with particular emphasis on displacement data for [3H]rauwolscine and the interaction with rauwolscine in isolated organs." @default.
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- W2012808016 date "1986-03-01" @default.
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- W2012808016 title "A reassessment of the binding of [3H]rauwolscine to membranes from the rat cortex" @default.
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- W2012808016 doi "https://doi.org/10.1016/0028-3908(86)90254-6" @default.
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