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首页> 外文期刊>Life sciences >Characterization of (3H)nisoxetine binding in rat vas deferens membranes: modulation by sigma and PCP ligands.
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Characterization of (3H)nisoxetine binding in rat vas deferens membranes: modulation by sigma and PCP ligands.

机译：大鼠输精管膜中（3H）尼西汀的结合特征：σ和PCP配体的调节。

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摘要

Sigma (sigma) and phencyclidine (PCP) receptor ligands, apart from their main effects on sigma receptors and NMDA receptor-mediated neurotransmission, have been found to interact with catecholamine systems in several central and peripheral tissues. In the present study the binding profile of [3H]nisoxetine ([3H]NIS), a selective marker of the noradrenaline transporter, has been characterized in rat vas deferens membranes to further study its modulation by a number of characteristic sigma and PCP ligands. The binding of [3H]NIS was found to be of high affinity (Kd = 1.63 +/- 0.36 nM), saturable, sodium-dependent and to a single population of binding sites (nH = 1.003 +/- 0.017). The maximal binding capacity was 1,625 +/- 500 fmol/mg of protein. Kinetic experiments gave a k(+1) of 3.9 x 10(7) min(-1)M(-1) and a k(-1) of 0.005 min(-1). The [3H]NIS binding was totally inhibited, with IC50 values in the micromolar range, by all the sigma and PCP ligands tested, with the following order of potency: haloperidol > dextromethorphan > dizocilpine > dextrorphan > (+)-3-PPP > PCP > tenocyclidine. This order correlates well with that described in other tissues using [3H]desmethylimipramine. The inhibition by all these compounds, except that of (+)-3-PPP, was competitive. These results suggest that sigma and PCP ligands bind, at low micromolar concentrations, to a site in the noradrenaline transporter that is labelled by [3H]NIS.
机译：除了它们对sigma受体和NMDA受体介导的神经传递的主要作用外，还发现了Sigma（sigma）和苯环利定（PCP）受体配体与几种中枢和外周组织中的儿茶酚胺系统相互作用。在本研究中，已在大鼠输精管膜中表征了去甲肾上腺素转运蛋白的选择性标记物[3H] nisoxetine（[3H] NIS）的结合概况，以进一步研究其通过许多特征sigma和PCP配体的调节作用。发现[3H] NIS的结合具有高亲和力（Kd = 1.63 +/- 0.36 nM），可饱和，钠依赖性且与单个结合位点群相关（nH = 1.003 +/- 0.017）。最大结合能力为1,625 +/- 500 fmol / mg蛋白质。动力学实验得出k（+1）为3.9 x 10（7）min（-1）M（-1）和k（-1）为0.005 min（-1）。 [3H] NIS结合被所有测试的sigma和PCP配体完全抑制，IC50值在微摩尔范围内，其效力依次为：氟哌啶醇>右美沙芬>地佐西平>右啡烷>（+）-3-PPP> PCP>替诺环定。该顺序与使用[3H]去甲基亚胺基丙胺的其他组织中描述的顺序非常相关。除（+）-3-PPP以外，所有这些化合物的抑制作用都是竞争性的。这些结果表明，sigma和PCP配体在低微摩尔浓度下与去甲肾上腺素转运蛋白上由[3H] NIS标记的位点结合。

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