Molecular cloning of a levocabastine-sensitive neurotensin binding site.
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.
Chalon
P
P
Sanofi Recherche, Labège Cedex, France.
Vita
N
N
Kaghad
M
M
Guillemot
M
M
Bonnin
J
J
Delpech
B
B
Le Fur
G
G
Ferrara
P
P
Caput
D
D
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
C099727:Ntsr2 protein, rat; D010880:Piperidines; D012333:RNA, Messenger; D018028:Receptors, Neurotensin; C047340:levocabastine