Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D
Sanofi Recherche, Labège Cedex, France.
FEBS Lett. 1996 May 20;386(2-3):91-4. doi: 10.1016/0014-5793(96)00397-3.
A search for sequences homologous to the neurotensin receptor cDNA in a rat hypothalamic library has identified a novel neurotensin receptor (NTR-2). The 1539 bp cDNA encodes a 416 amino acid protein and shows highest homology to the previously cloned neurotensin receptor (NTR-1) (64% homology and 43% identity). Binding and pharmacological studies demonstrate that NTR-2 expressed in COS cells recognizes neurotensin (NT) with high affinity as well as several other agonists and antagonists. However, a fundamental difference was found; unlike NTR-1, NTR-2 recognizes, with high affinity, levocabastine, a histamine H1 receptor antagonist previously shown to compete with NT for low-affinity binding sites in brain.
在大鼠下丘脑文库中搜索与神经降压素受体cDNA同源的序列时，鉴定出一种新型神经降压素受体（NTR-2）。这个1539 bp的cDNA编码一个416个氨基酸的蛋白质，与先前克隆的神经降压素受体（NTR-1）具有最高的同源性（64%同源性和43%同一性）。结合和药理学研究表明，在COS细胞中表达的NTR-2以高亲和力识别神经降压素（NT）以及其他几种激动剂和拮抗剂。然而，发现了一个根本差异；与NTR-1不同，NTR-2以高亲和力识别左卡巴斯汀，一种组胺H1受体拮抗剂，先前已证明它能与NT竞争脑中的低亲和力结合位点。
