title: SR 48692 inhibits neurotensin-induced [3H]dopamine release in rat striatal slices and mesencephalic cultures.
abstract: In rat striatal slices, the increase (114 +/- 11%) in K(+)-evoked [3H]dopamine release induced by neurotensin (10 nM) was antagonized by 2-[(1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl) carboxylamino]tricyclo(3.3.1.1.3.7)decan-2-carboxylic acid (SR 48692, IC50 = 1.2 +/- 0.11 nM). SR 48692 (100 nM) also suppressed the neurotensin (10 nM)-induced increase (47%) in K(+)-evoked [3H]dopamine release in primary cultures of fetal rat mesencephalic cells. These results further characterize SR 48692 as a potent antagonist of neurotensin receptors in the rat.
authors.affiliation: Institut National de la Santé et de la Recherche Médicale, Unité 339, Hôpital Saint Antoine, Paris, France.
authors.forename: A
authors.initials: A
authors.lastname: Brouard
authors.forename: M
authors.initials: M
authors.lastname: Heaulme
authors.forename: R
authors.initials: R
authors.lastname: Leyris
authors.forename: D
authors.initials: D
authors.lastname: Pelaprat
authors.forename: D
authors.initials: D
authors.lastname: Gully
authors.forename: P
authors.initials: P
authors.lastname: Kitabgi
authors.forename: G
authors.initials: G
authors.lastname: Le Fur
authors.forename: W
authors.initials: W
authors.lastname: Rostene
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D008297:Male; D008636:Mesencephalon / Q000166:cytology / Q000187:drug effects* / Q000196:embryology; D009496:Neurotensin / Q000494:pharmacology; D011720:Pyrazoles / Q000494:pharmacology*; D011804:Quinolines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D018028:Receptors, Neurotensin / Q000037:antagonists & inhibitors
chemical_list: D011720:Pyrazoles; D011804:Quinolines; D018028:Receptors, Neurotensin; C079087:SR 48692; D009496:Neurotensin; D004298:Dopamine