Yamada J, Sugimoto Y
Department of Pharmacology, Kobe Pharmaceutical University, Motoyamakita-machi, Higashinada, Kobe 658-8558, Japan.
Eur J Pharmacol. 2001 Sep 21;427(3):221-5. doi: 10.1016/s0014-2999(01)01240-7.
The effects of 5-HT(2) receptor antagonists on antidepressant effects of imipramine were investigated in the forced swimming test. Imipramine induced anti-immobility effects in mice dose dependently. Pretreatment with the 5-HT(2A/2B/2C) receptor antagonist, 4-isopropyl-7-methyl-9-(2-hydroxy-1-methyl-propoxycarbonyl)-4,6A,7,8,9,10,10A-octahydro-indolo[4,3-FG]quinolone maleate (LY 53857) significantly enhanced the anti-immobility effects of imipramine. The 5-HT(2C/2B) receptor antagonist, N-3-pyridinyl-3,5-dihydro-5-methyl-benzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide (SB 206553), also enhanced, while the 5-HT(2A) receptor antagonist, ketanserin, was without effect. These results suggest that blockade of the 5-HT(2C/2B) receptor leads to potentiation of the antidepressant effects of imipramine.
在强迫游泳试验中研究了5-羟色胺(5-HT)(2)受体拮抗剂对丙咪嗪抗抑郁作用的影响。丙咪嗪对小鼠的抗不动效应呈剂量依赖性。用5-HT(2A/2B/2C)受体拮抗剂马来酸4-异丙基-7-甲基-9-(2-羟基-1-甲基-丙氧基羰基)-4,6A,7,8,9,10,10A-八氢-吲哚并[4,3-FG]喹诺酮(LY 53857)预处理可显著增强丙咪嗪的抗不动效应。5-HT(2C/2B)受体拮抗剂N-3-吡啶基-3,5-二氢-5-甲基-苯并[1,2-b:4,5-b']二吡咯-1(2H)-甲酰胺(SB 206553)也有增强作用,而5-HT(2A)受体拮抗剂酮色林则无此作用。这些结果表明,阻断5-HT(2C/2B)受体可增强丙咪嗪的抗抑郁作用。