title: Increase in neurotensin receptor expression in rat brain induced by chronic treatment with the nonpeptide neurotensin receptor antagonist SR 48692.
abstract: In the present study, we examined the regulation of neurotensin receptor following a chronic pharmacological blockade of the neurotensin transmission with a nonpeptide neurotensin receptor antagonist, SR 48692. Our results showed that treatment of the rats for five days with SR 48692, at a dose of 1 mg/kg, i.p., induced an increase of both the number of binding sites for 125I-neurotensin to whole brain membrane homogenates and neurotensin receptor mRNA levels in the ventral mesencephalon. This study brings the first evidence for an in vivo up-regulation of neurotensin receptors following their pharmacological blockade, and suggests that endogenous neurotensin exerts a tonic inhibitory control on neurotensin receptor mRNA levels.
authors.affiliation: INSERM U339, Hôpital Saint-Antoine, Paris, France.
authors.forename: M
authors.initials: M
authors.lastname: Azzi
authors.forename: A
authors.initials: A
authors.lastname: Nicot
authors.forename: D
authors.initials: D
authors.lastname: Gully
authors.forename: P
authors.initials: P
authors.lastname: Kitabgi
authors.forename: A
authors.initials: A
authors.lastname: Bérod
authors.forename: W
authors.initials: W
authors.lastname: Rostène
mesh_terms: D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects*; D003720:Densitometry; D017403:In Situ Hybridization; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D009496:Neurotensin / Q000493:pharmacokinetics; D011720:Pyrazoles / Q000494:pharmacology*; D011804:Quinolines / Q000494:pharmacology*; D012333:RNA, Messenger / Q000096:biosynthesis; D051381:Rats; D017208:Rats, Wistar; D018028:Receptors, Neurotensin / Q000037:antagonists & inhibitors* / Q000096:biosynthesis*
chemical_list: D007457:Iodine Radioisotopes; D011720:Pyrazoles; D011804:Quinolines; D012333:RNA, Messenger; D018028:Receptors, Neurotensin; C079087:SR 48692; D009496:Neurotensin