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Molecular cloning of a levocabastine‐sensitive neurotensin binding site
Author(s) -
Chalon Pascale,
Vita Natalio,
Kaghad Mourad,
Guillemot Marie,
Bonnin Jacques,
Delpech Bruno,
Le Fur Gerard,
Ferrara Pascual,
Caput Daniel
Publication year - 1996
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(96)00397-3
Subject(s) - neurotensin , cloning (programming) , chemistry , binding site , molecular cloning , biochemistry , peptide sequence , gene , neuropeptide , receptor , computer science , programming language
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.