[3H]quipazine labels 5-HT3 recognition sites in rat cortical membranes.

[3H]quipazine labels 5-HT3 recognition sites in rat cortical membranes.
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[3H]quipazine 标记大鼠皮质膜中的 5-HT3 识别位点。

DOI:
10.1016/0014-2999(88)90579-1
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发表时间:
1988
影响因子:
5
通讯作者:
Hamik,A
Hamik,A
中科院分区:
医学2区
文献类型:
--
作者:
Peroutka,SJ;Hamik,A

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5-羟色胺(5-HT)受体在外周神经系统中已被广泛表征,它们似乎介导5-HT的兴奋作用(Richardson和Engel,1986)。最近,有人提出这些受体也存在于中枢神经系统中。事实上,已经报道[3 H] GR 65630标记大鼠皮质膜中假定的5-HT 1受体(Kilpatrick等人,1987)和[3 H] ICS 205-930标记成神经细胞瘤-神经胶质瘤细胞系中的表观5-HT 1受体(Hoyer和Neijt,1987)。由于喹帕嗪对外周5-HT受体的有效拮抗作用(爱尔兰和Tyers,1987; Round和沃利斯,1987),我们分析了[3 H]喹帕嗪标记大鼠皮质膜中表观5-HT识别位点的能力。(1987年)。简言之,将大鼠皮质(Pel Freeze Biologicals; Rogers,AR)在20体积试验缓冲液中匀浆,并以49000 xg离心10 min。弃去上清液,将沉淀物重悬于相同体积的缓冲液中。在37 ° C下孵育10分钟后,将组织第二次离心。将最终沉淀重悬于80体积测定缓冲液中。结合试验由0.1 ml [3 H]喹帕嗪(DuPont新英格兰核能公司; Boston,MA)、0.1 ml置换药物和0.8 ml组织匀浆组成。福尔-
5-Hydroxytryptamine,(5-HT,) receptors have been extensively characterized in the peripheral nervous system where they appear to mediate the excitatory effects of 5-HT (Richardson and Engel, 1986). More recently, it has been suggested that these receptors also exist in the central nervous system. Indeed,[3H] GR 65630 has been reported to label putative 5-HT, receptors in rat cortical membranes (Kilpatrick et al., 1987) and [3H] ICS 205-930 labels an apparent 5-HT, receptor in a neuroblastoma-glioma cell line (Hoyer and Neijt, 1987). Due to the potent antagonist effects of quipazine at peripheral 5-HT, receptors (Ireland and Tyers, 1987; Round and Wallis, 1987) we have analyzed the ability of [3H] quipazine to label apparent 5-HT, recognition sites in rat cortical membranes.Radioligand binding assays were performed according to the methods of Kilpatrick et al.(1987). Briefly, rat cortex (Pel Freeze Biologicals; Rogers, AR) was homogenized in 20 volume assay buffer and centrifuged at 49000 xg for 10 min. The supernatant was discarded and the pellet resuspended in the same volume of buffer. After a 10 min incubation at 37’C, the tissue was centrifuged for a second time. The final pellet was resuspended in 80 volume assay buffer. Binding assays consisted of 0.1 ml [3H] quipazine (DuPont New England Nuclear; Boston, MA), 0.1 ml displacing drug and 0.8 ml tissue homogenate. Fol-