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Volume 16, Number 18, Issue of September 15, 1996 pp. 5613-5620
Copyright ©1996 Society for NeuroscienceStructure, Functional Expression, and Cerebral Localization of the Levocabastine-Sensitive Neurotensin/Neuromedin N Receptor from Mouse Brain
Received March 13, 1996; revised June 14, 1996; accepted June 27, 1996.
Jean Mazella, Jean-Marie Botto, Eric Guillemare, Thierry Coppola, Philippe Sarret, and Jean-Pierre Vincent Institut de Pharmacologie Moléculaire et Cellulaire, Unité Propre de Recherche 411, Centre National de la Recherche Scientifique, 06560 Valbonne, France
This work describes the cloning and expression of the levocabastine-sensitive neurotensin (NT) receptor from mouse brain. The receptor protein comprises 417 amino acids and bears the characteristics of G-protein-coupled receptors. This new NT receptor (NTR) type is 39% homologous to, but pharmacologically distinct from, the only other NTR cloned to date from the rat brain and the human HT29 cell line. When the receptor is expressed in Xenopus laevis oocytes, the H1 antihistaminic drug levocabastine, like NT and neuromedin N, triggers an inward current. The pharmacological properties of this receptor correspond to those of the low-affinity, levocabastine-sensitive NT binding site described initially in membranes prepared from rat and mouse brain. It is expressed maximally in the cerebellum, hippocampus, piriform cortex, and neocortex of adult mouse brain.
Key words: neurotensin; neuromedin N; receptor; levocabastine; cloning; low affinity; G-protein-coupled
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