对α7烟碱受体具有高亲和力且与5-HT3受体无交叉反应性的配体。
High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor.
作者信息
Baker S Richard, Boot John, Brunavs Michael, Dobson David, Green Rachel, Hayhurst Lorna, Keenan Martine, Wallace Louise
机构信息
Eli Lilly and Company Ltd., Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK.
出版信息
Bioorg Med Chem Lett. 2005 Nov 1;15(21):4727-30. doi: 10.1016/j.bmcl.2005.07.070.
Potent and selective ligands of the alpha7 nicotinic acetylcholine receptor are required to understand the pharmacological effect of alpha7 activation. A common cross-reactivity occurs with serotonergic 5-HT3 receptors with which alpha7 receptors have a high sequence homology. We demonstrate that certain quinuclidine 3-biaryl carboxamides are high affinity alpha7 ligands with an excellent binding selectivity over 5-HT3 receptors.
需要α7烟碱型乙酰胆碱受体的强效和选择性配体来了解α7激活的药理作用。与α7受体具有高序列同源性的血清素能5-HT3受体存在常见的交叉反应性。我们证明，某些奎宁环3-联芳基羧酰胺是高亲和力的α7配体，对5-HT3受体具有优异的结合选择性。
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