X-ray structural characterization of SR 142948, a novel potent synthetic neurotensin receptor antagonist

SR 142948 is an original and extremely potent neurotensin receptor antagonist developped in a promising approach to novel antipsychotic drugs. The X-ray structure was elucidated and compared to SR 48692 and levocabastine, providing new informations about the possible recognition process of NT recept...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-03, Vol.8 (6), p.653-658
Hauptverfasser:	Quéré, Luc, Longfils, Géraldine, Boigegrain, Robert, Labeeuw, Bernard, Gully, Danielle, Durant, François
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Crystallography, X-Ray Medical sciences Mice Models, Molecular Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Piperidines - chemistry Protein Conformation Pyrazoles - chemistry Pyrazoles - pharmacology Quinolines - chemistry Quinolines - pharmacology Rats Receptors, Neurotensin - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	SR 142948 is an original and extremely potent neurotensin receptor antagonist developped in a promising approach to novel antipsychotic drugs. The X-ray structure was elucidated and compared to SR 48692 and levocabastine, providing new informations about the possible recognition process of NT receptor subtypes. The X-ray structure of SR 142948, an original and potent neurotensin (NT) receptor antagonist was elucidated and compared to SR 48692 and levocabastine, providing new informations about the possible recognition process of NT receptor subtypes.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00087-0