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The Journal of Neuroscience, January 1, 1999, 19(1):503-510
Identification of the Receptor Subtype Involved in the Analgesic
Effect of Neurotensin
Isabelle
Dubuc1,
Philippe
Sarret2,
Catherine
Labbé-Jullié2,
Jean-Marie
Botto2,
Eric
Honoré2,
Elisabeth
Bourdel3,
Jean
Martinez3,
Jean
Costentin1,
Jean-Pierre
Vincent2,
Patrick
Kitabgi2, and
Jean
Mazella2
1 Unité de Neuropsychopharmacologie
Expérimentale, Centre National de la Recherche Scientifique
(CNRS), 76803 Saint Etienne du Rouvray, France, 2 Institut
de Pharmacologie Moléculaire et Cellulaire, CNRS, 06560 Valbonne,
France, and 3 Laboratoire des Aminoacides, Peptides et
Protéines, ESA CNRS, Faculté de Pharmacie,
Universités de Montpellier 1 et 2, 34060 Montpellier,
France.
The neuropeptide neurotensin (NT) elicits hypothermic and
naloxone-insensitive analgesic responses after brain injection. Recent
pharmacological evidence obtained with NT agonists and antagonists
suggests that these effects are mediated by a receptor distinct from
the initially cloned high-affinity NT receptor (NTR1). The recent
cloning of a second NT receptor (NTR2) prompted us to evaluate its role
in NT-induced analgesia. Intracerebroventricular injections in mice of
two different antisense oligodeoxynucleotides from the NTR2 markedly
decreased NTR2 mRNA and protein and reduced NT-induced analgesia. This
effect was specific, because NTR1 levels were unaffected, and sense or
scramble oligodeoxynucleotides had no effect. Structure-activity
studies revealed a close correlation between the analgesic potency of
NT analogs and their affinity for the NTR2 and disclosed potent and
selective agonists of this receptor. These data confirm that NTR1 is
involved in the NT-elicited turning behavior and demonstrate that the
NTR2 mediates NT-induced analgesia.
Key words:
analgesia; neurotensin; receptor; levocabastine-sensitive; oligodeoxynucleotide; antisense
Copyright © 1999 Society for Neuroscience 0270-6474/99/191503-08$05.00/0
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