Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain.
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.
Mazella
J
J
Institut de Pharmacologie Moléculaire et Cellulaire, Unité Propre de Recherche 411, Centre National de la Recherche Scientifique, Valbonne, France.
Botto
J M
JM
Guillemare
E
E
Coppola
T
T
Sarret
P
P
Vincent
J P
JP
D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D001921:Brain / Q000378:metabolism*; D003001:Cloning, Molecular; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D009496:Neurotensin / Q000378:metabolism*; D010446:Peptide Fragments / Q000378:metabolism*; D010880:Piperidines / Q000494:pharmacology*; D012333:RNA, Messenger / Q000378:metabolism; D051381:Rats; D018028:Receptors, Neurotensin / Q000235:genetics / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014982:Xenopus laevis
D006634:Histamine H1 Antagonists; D010446:Peptide Fragments; D010880:Piperidines; D012333:RNA, Messenger; D018028:Receptors, Neurotensin; C042090:neuromedin N; D009496:Neurotensin; C047340:levocabastine