Isolation and Characterization of an Endogenous Peptide from Rat Brain Interacting Specifically with the Serotonergic 1B Receptor Subtypes (*)
Isolation and Characterization of an Endogenous Peptide from Rat Brain Interacting Specifically with the Serotonergic 1B Receptor Subtypes (*)
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与血清素 1B 受体亚型特异性相互作用的大鼠脑内源性肽的分离和表征 (*)
DOI：
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发表时间：
1996
影响因子：
4.8
通讯作者：
G. Fillion
中科院分区：
文献类型：
--
作者：
J. Rousselle;O. Massot;M. Delepierre;E. Zifa;B. Rousseau;G. Fillion
先前假设存在与α-肾上腺素能系统相互作用的内源性化合物。本研究采用酸性和有机溶剂法提取大鼠脑组织。测试所得提取物与[3 H]5-羟色胺（[3 H]5-HT）结合5-HT 1受体的相互作用能力。通过高压液相色谱法分离和纯化负责观察到的抑制活性的化合物。鉴定了一个新的氨基酸序列Leu-Ser-Ala-Leu（LSAL）的四肽。在低浓度下，它降低[3 H]5-HT与5-HT 1受体的结合（IC 50 = 10− 10 M）。这种效应对应于5-HT 1B受体的特异性相互作用，因为LSAL不会显著影响其他神经递质结合。LSAL在整个脑（海马>小脑>纹状体>脑干）和外周组织（肾>肺>胃>血液>肝>脾）中呈现不均匀分布。还纯化了另外两种肽，Leu-Ser（LS）和Ala-Leu（AL）。与LSAL相比，它们几乎不影响[3 H]5-HT结合。它们可能代表功能肽LSAL的降解产物。LSAL与5-HT 1B受体特异性相互作用的事实表明，该肽可能参与控制5-HT神经传递的机制，因此，可能在与5-HT活性相关的病理生理功能中发挥重要作用，5-HT 1B受体抑制神经递质的释放，特别是5-HT本身的释放。
The existence of endogenous compounds interacting with the serotonergic system was previously postulated. In the present work, rat brain tissues were extracted by acidic and organic procedures. The resulting extract was tested for its capacity to interact with the binding of [3H]5-hydroxytryptamine ([3H]5-HT) to 5-HT1 receptors. Compounds responsible for the observed inhibitory activities were isolated and purified by high pressure liquid chromatography. A tetrapeptide corresponding to a novel amino acid sequence Leu-Ser-Ala-Leu (LSAL) was identified. It reduces the binding of [3H]5-HT to 5-HT1 receptors at low concentration (IC50 = 10−10M). This effect corresponds to a specific interaction at 5-HT1B receptors since LSAL does not significantly affect other neurotransmitter bindings. LSAL appears heterogeneously distributed throughout the brain (hippocampus > cerebellum > striatum > brain stem) and in peripheral tissues (kidney > lung > stomach > blood > liver > spleen). Two other peptides, Leu-Ser (LS) and Ala-Leu (AL), were also purified. They hardly affected [3H]5-HT binding compared with LSAL. They presumably represent degradation products of the functional peptide LSAL. The fact that LSAL interacts specifically with 5-HT1B receptors that inhibit the release of neurotransmitters and particularly that of 5-HT itself suggests that this peptide may be involved in mechanisms controlling 5-HT neurotransmission and, accordingly, may play an important role in pathophysiological functions related to 5-HT activity.
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OK 细胞（一种来自负鼠的肾上皮细胞系）中与腺苷酸环化酶负偶联的 5-羟色胺-1B 受体的表征。
DOI：
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发表时间：
1989
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Murphy,TJ;Bylund,DB
通讯作者：
Bylund,DB
血清素消耗揭示了大鼠脑中[3H]二氢阿普洛尔结合的血清素能成分。
影响因子：
3.6
作者：
Stockmeier,CA;Kellar,KJ
通讯作者：
Kellar,KJ
[3H]DOB：5-HT2 血清素受体的特异性激动剂放射性配体。
影响因子：
5
作者：
Titeler,M;Herrick,K;Lyon,RA;McKenney,JD;Glennon,RA
通讯作者：
Glennon,RA
大鼠 5-羟色胺 1B 受体是人类 5-羟色胺 1D β 受体的物种同源物。
影响因子：
3.6
作者：
Adham,N;Romanienko,P;Hartig,P;Weinshank,RL;Branchek,T
通讯作者：
Branchek,T
小鼠肾脏中的 G 蛋白连接血清素受体与大脑中的 5-HT1b 受体表现出相同的特性。
DOI：
--
发表时间：
1990
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Ciaranello,RD;Tan,GL;Dean,R
通讯作者：
Dean,R