Molecular cloning of a levocabastine-sensitive neurotensin binding site.

Article Details

Citation

Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D

Molecular cloning of a levocabastine-sensitive neurotensin binding site.

FEBS Lett. 1996 May 20;386(2-3):91-4.

PubMed ID
8647296 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
LevocabastineHistamine H1 receptorProteinHumans
Yes
Antagonist
Details
LevocabastineNeurotensin receptor type 2ProteinHumans
Yes
Partial antagonist
Details