[Neurotensin receptor antagonists and therapeutical perspectives].
SR 48692 is the first non-peptide antagonist of neurotensin receptors. It is potent and selective vs the high-affinity binding sites and with a small activity on the levocabastine-sensitive binding sites. It is active on several species including man without partial agonist properties. In vivo, it is active by oral route with a long duration of action and it is able to cross the blood-brain barrier. As an antagonist of neurotensin receptors, SR 48692 modulates central dopaminergic neurons. Thus it might be considered as a good tool for investigating the pathophysiological role of neurotensin in psychiatric diseases.
Gully
D
D
Sanofi Recherche, Toulouse, France.
Maffrand
J P
JP
Soubrié
P
P
Rostène
W
W
Kitabgi
P
P
Le Fur
G
G
D000818:Animals; D004298:Dopamine / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D009474:Neurons / Q000378:metabolism; D011720:Pyrazoles / Q000494:pharmacology*; D011804:Quinolines / Q000494:pharmacology*; D018028:Receptors, Neurotensin / Q000037:antagonists & inhibitors* / Q000187:drug effects
D011720:Pyrazoles; D011804:Quinolines; D018028:Receptors, Neurotensin; C079087:SR 48692; D004298:Dopamine
Antagonistes des récepteurs de la neurotensine et perspectives thérapeutiques.