[3H]-8-OH-DPAT binding in the rat brain raphe area:: involvement of 5-HT1A and non-5-HT1A receptors
[3H]-8-OH-DPAT binding in the rat brain raphe area:: involvement of 5-HT1A and non-5-HT1A receptors
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DOI：
10.1038/sj.bjp.0703426
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发表时间：
2000-07-01
影响因子：
7.3
通讯作者：
Koek, W
中科院分区：
文献类型：
--
作者：
Assié, MB;Koek, W
5-HT1A激动剂8-OH-DPAT已被证明具有额外的5-HT摄取抑制特性。本研究旨在进一步研究[H-3]-8-OH-DPAT在大鼠大脑中叶区的结合，该区域富含5-HT1A受体和5-HT摄取位点。2 5-HT以双相方式抑制[H-3]-8-OH-DPAT结合(pK(i1): 8.82+/-0.01, pK(i2): 6.07+/-0.05, n=4)，低亲和力位点占总数的36+/-4%。5-HT1A拮抗剂WAY 100635也存在双相抑制曲线(pK（i1): 8.65+/-0.17, pK(i2): 4.26+/-0.38, n=3）。在1 μ M WAY 100635存在的情况下，5-HT以单相方式抑制[H-3]-8-OH-DPAT结合（pK(i): 6.04+/-0.07, n=3）测定了不同化合物在1 μ M WAY 100635存在时对[H-3]-8-OH-DPAT标记的位点和[H-3]-西酞普兰（一种选择性5-羟色胺摄取抑制剂）标记的位点的亲和力。5-HT摄取位点和[H-3]-8-OH-DPAT标记的非5ht （1A）位点的pK(i)值之间存在显著相关性(r=0.80， P
The 5-HT1A agonist 8-OH-DPAT has been shown to have additional 5-HT uptake inhibiting properties. The present work was undertaken to examine further the binding of [H-3]-8-OH-DPAT in the raphe area of the rat brain, a region rich in 5-HT1A receptors and 5-HT uptake sites.2 5-HT inhibited [H-3]-8-OH-DPAT binding in a biphasic manner (pK(i1): 8.82+/-0.01, pK(i2): 6.07+/-0.05, n=4) with the low affinity site representing 36+/-4% of the total population. A biphasic inhibition curve was found also with the 5-HT1A antagonist, WAY 100635 (pK(i1): 8.65+/-0.17, pK(i2): 4.26+/-0.38, n=3). In the presence of 1 mu M WAY 100635 to mask 5-HT1A receptors, 5-HT inhibited [H-3]-8-OH-DPAT binding in a monophasic manner (pK(i): 6.04+/-0.07, n=3).3 The affinities of various compounds for sites labelled by [H-3]-8-OH-DPAT in the presence of 1 mu M WAY 100635 and for sites labelled by [H-3]-citalopram (a selective 5-HT uptake inhibitor) were determined. There was a significant correlation between pK(i) values at 5-HT uptake sites and at non-5HT(1A) sites labelled by [H-3]-8-OH-DPAT (r=0.80, P