Effect of the 5-HT3 receptor antagonist, GR38032F, on responses to injection of a neurokinin agonist into the ventral tegmental area of the rat brain.
Effect of the 5-HT3 receptor antagonist, GR38032F, on responses to injection of a neurokinin agonist into the ventral tegmental area of the rat brain.
复制标题
5-HT3 受体拮抗剂 GR38032F 对向大鼠大脑腹侧被盖区注射神经激肽激动剂的反应的影响。
DOI：
10.1016/0014-2999(87)90450-x
复制
发表时间：
1987
影响因子：
5
通讯作者：
M. Tyers
中科院分区：
文献类型：
--
作者：
R. Hagan;Arthur Butler;Julia M. Hill;C. Jordan;S. J. Ireland;M. Tyers
最近，已经报道了GR 38032 F（1，2，3，9-四氢-9-甲基-3-[（2-甲基咪唑-1-基）甲基]咔唑-4-酮，盐酸盐，二水合物），一种有效的和选择性的5-HT 3受体拮抗剂（Brittain等人，1987），可以减少将多巴胺长期输注到大鼠和绒猴的中脑边缘核的行为后果（Costall等，1987年）。我们现在报道了GR 38032 F对大鼠中的活动过度反应的影响，该反应是由将神经激肽受体激动剂[pGluS，MePheS，Sarg] sP-（5-11）（DiMe-C7）注射到中脑的腹侧被盖区（VTA）中引起的（Eison等人，1982年）。这种行为变化伴随着前脑的中脑边缘和中皮层区域中多巴胺代谢的增加（Elliot等人，1986），被认为是由投射到这些额叶区域的多巴胺能A10神经元的细胞体的激活引起的。因此，我们还确定了GR 38032 F对DiMe-C7诱导的中脑边缘核多巴胺和5-HT及其代谢物水平变化的影响。
Recently, it has been reported that GR38032F (1, 2, 3, 9-tetrahydro-9-methyl-3-[(2-methylimidazol-1-yl) methyl] carbazole-4-one, hydrochloride, dihydrate), a potent and selective antagonist at 5-HT 3 receptors (Brittain et al., 1987), can reduce the behavioural consequences of chronic infusion of dopamine into the mesolimbic nucleus accumbens of the rat and marmoset (Costall et al., 1987). We now report the effect of GR38032F on a hyperactivity response in rats which results from injection of the neurokinin receptor agonist,[pGluS, MePheS, Sarg] sP-(5-11)(DiMe-C7), into the ventral tegmental area (VTA) of the midbrain (Eison et al., 1982). This behavioural change, which is accompanied by increases in dopamine metabolism in the mesolimbic and mesocortical areas of the forebrain (Elliot et al., 1986), is thought to arise from activation of the cell bodies of the dopaminergic A10 neurones which project to these frontal areas. Therefore, we have also determined the effect of GR38032F on DiMe-C7-induced changes in the levels of dopamine and 5-HT and their metabolites in the mesolimbic nucleus accumbens.