Nucleotide interactions with 5-HT1A binding sites directly labeled by [3H]-8-hydroxy-2-(DI-n-propylamino)tetralin ([3H]-8-OH-DPAT).
Nucleotide interactions with 5-HT1A binding sites directly labeled by [3H]-8-hydroxy-2-(DI-n-propylamino)tetralin ([3H]-8-OH-DPAT).
复制标题
与直接由 [3H]-8-羟基-2-(二正丙氨基)四氢萘 ([3H]-8-OH-DPAT) 标记的 5-HT1A 结合位点的核苷酸相互作用。
DOI：
10.1016/0006-2952(86)90725-2
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发表时间：
1986
影响因子：
5.8
通讯作者：
Peroutka,SJ
中科院分区：
文献类型：
--
作者：
Schlegel,JR;Peroutka,SJ
用8-OH-DPAT标记5-羟色胺1A（5-HT 1A）结合位点，研究核苷酸间的相互作用。在10− 4 M浓度下，GTP和GDP使0.4 nM [3 M]-8-OH-DPAT的特异性结合分别降低至对照值的47±4和61±1%。这种核苷酸效应显著大于（P< 0.005）在1.5nM [3 H]-5-HT标记的总5-HT 1结合位点处观察到的效应。浓度低于10− 3 M时，GMP和腺嘌呤核苷酸对[3 H]-8-OH-DPAT结合的影响极小。饱和实验表明，10− 4 M GTP增加了[3 H]-8-OH-DPAT对5-HT 1A结合位点的KD（0.79至2.7 nM），而不改变结合位点的数量（1.98至1.93 pmole/g组织）。在10− 4 M GTP存在下，经典和新型推定的5-HT激动剂的Ki值增加2- 4倍。5-HT拮抗剂对[3 H]-8-OH-DPAT位点的亲和力不受在结合试验中加入10− 4 M GTP的影响。
Nucleotide interactions were examined at 5-hydroxytryptamine 1A (5-HT 1A) binding sites labeled by [3 H]-8-hydroxy-2-(di)-n-propylamino) tetralin (8-OH-DPAT). At a 10− 4 M concentration, GTP and GDP decreased specific binding of 0.4 nM [3 M]-8-OH-DPAT to 47±4 and 61±1% of control values respectively. This nucleotide effect was significantly greater (P< 0.005) than observed at total 5-HT 1 binding sites labeled by 1.5 nM [3 H]-5-HT. GMP and adenine nucleotides had a minimal effect on [3 H]-8-OH-DPAT binding at concentrations less than 10− 3 M. Saturation experiments demonstrated that 10− 4 M GTP increased the K D of [3 H]-8-OH-DPAT for 5-HT 1A binding sites (0.79 to 2.7 nM) without changing the number of binding sites (1.98 to 1.93 pmoles/g tissue). The K i vlaues of classic and novel putative 5-HT agonists were increased 2-to 4-fold in the presence of 10− 4 M GTP. Affinities of 5-HT antagonists for the [3 H]-8-OH-DPAT site were not affected by the addition of 10− 4 M GTP to the binding assay.