8-[H-3]HYDROXY-2-(DI-N-PROPYLAMINO) TETRALIN BINDING-SITES IN GOLDFISH RETINA
8-[H-3]HYDROXY-2-(DI-N-PROPYLAMINO) TETRALIN BINDING-SITES IN GOLDFISH RETINA
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DOI：
10.1007/bf00971572
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发表时间：
1994-03-01
影响因子：
4.4
通讯作者：
URBINA, M
中科院分区：
文献类型：
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作者：
LIMA, L;SCHMEER, C;URBINA, M
研究了8-[H-3]羟基-2-(二正丙氨基)四氢萘([H-3]DPAT)在金鱼视网膜中的结合部位，以评价该配体对5-羟色胺(1A)(5HT(1A))受体的选择性。结合的特异性是在5-羟色胺和多巴胺能激动剂和拮抗剂存在的情况下进行的。丁螺环酮、螺环素和5-甲氧基-N，N-二甲基色胺的抑制作用最强，其次是心得安、西酞普兰、丙咪嗪和地昔帕明。5-羟色胺不是一种有效的抑制剂，它与[H-3]DPAT结合部位的相互作用是复杂的。诺米芬辛表现出重要的抑制作用，然而，其他多巴胺摄取阻滞剂，如安非他酮和GBR-12909，效力较弱。氟哌啶醇也是一种很好的抑制剂，但D-1受体激动剂SKF-38393、D-2受体拮抗剂舒必利和多巴胺不抑制这种结合。GppNHp在微摩尔范围内抑制结合。用丁螺环酮确定非特异性结合，用同位素稀释法进行饱和实验分析，揭示了两个位点。丁螺环酮定义的结合位点数高于诺米芬新定义的结合位点数。以丁螺环酮为定义的特异性结合可通过眼内注射6-羟基多巴胺而减少。这项研究表明，[H-3]DPAT标记了金鱼视网膜中的5HT(1A)受体，但也与非5HT受体部位相互作用。这些受体似乎定位于多巴胺能神经元。
The binding sites of 8-[H-3]hydroxy-2-(di-n-propylamino)tetralin ([H-3]DPAT) were characterized in the retina of goldfish in order to evaluate the selectivity of the ligand for serotonin(1A) (5HT(1A)) receptors. Specificity of the binding was performed in the presence of serotonergic and dopaminergic agonists and antagonists. Buspirone, spiroxatrine and 5-methoxy-N,N-dimethyltryptamine were potent inhibitors, followed by propranolol, citalopram, imipramine and desipramine. Serotonin was not a potent inhibitor, and its interaction with the binding sites of [H-3]DPAT was complex. Nomifensine displayed an important inhibition, however, other dopamine uptake blockers, such as bupropion and GBR-12909, were less potent. Haloperidol was also a good inhibitor, but the D-1 receptor agonist, SKF-38393, the D-2 receptor antagonist, sulpiride, and dopamine did not inhibit the binding. GppNHp inhibited the binding in the micromolar range. The analysis of saturation experiments by isotopic dilution, using buspirone to determine nonspecific binding, revealed two sites. The number of binding sites defined by buspirone were higher than the ones defined by nomifensine. The specific binding, using buspirone for definition, was reduced by the intraocular injection of 6-hydroxydopamine. This investigation demonstrates that [H-3]DPAT labels 5HT(1A) receptors in goldfish retina, but also interacts with a non-5HT receptor site. These receptors seem to be localized in dopaminergic neurons.