title: Molecular cloning of a levocabastine-sensitive neurotensin binding site.
abstract: 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.
authors.affiliation: Sanofi Recherche, Labège Cedex, France.
authors.forename: P
authors.initials: P
authors.lastname: Chalon
authors.forename: N
authors.initials: N
authors.lastname: Vita
authors.forename: M
authors.initials: M
authors.lastname: Kaghad
authors.forename: M
authors.initials: M
authors.lastname: Guillemot
authors.forename: J
authors.initials: J
authors.lastname: Bonnin
authors.forename: B
authors.initials: B
authors.lastname: Delpech
authors.forename: G
authors.initials: G
authors.lastname: Le Fur
authors.forename: P
authors.initials: P
authors.lastname: Ferrara
authors.forename: D
authors.initials: D
authors.lastname: Caput
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002460:Cell Line; D002522:Chlorocebus aethiops; D007031:Hypothalamus / Q000378:metabolism; D008969:Molecular Sequence Data; D010880:Piperidines / Q000494:pharmacology*; D012333:RNA, Messenger; D051381:Rats; D018028:Receptors, Neurotensin / Q000187:drug effects / Q000235:genetics* / Q000378:metabolism; D017386:Sequence Homology, Amino Acid; D014018:Tissue Distribution
chemical_list: C099727:Ntsr2 protein, rat; D010880:Piperidines; D012333:RNA, Messenger; D018028:Receptors, Neurotensin; C047340:levocabastine