Macor J E, Gurley D, Lanthorn T, Loch J, Mack R A, Mullen G, Tran O, Wright N, Gordon J C
AstraZeneca, Three Biotech, Worcester, MA 01605, USA.
Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21. doi: 10.1016/s0960-894x(00)00670-3.
The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropisetron were also found to be potent and selective partial agonists at alpha7 nicotinic receptors.
5-羟色胺3(5-HT3)受体拮抗剂托烷司琼(ICS 205-930)被发现是α7烟碱样受体的一种强效且选择性的部分激动剂。另外两种5-HT3受体拮抗剂昂丹司琼和LY-278,584,被发现对α7烟碱样受体缺乏高亲和力。托烷司琼的奎宁环类似物(1和2)也被发现是α7烟碱样受体的强效且选择性的部分激动剂。