Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.

Malherbe, Pari; Kratzeisen, Claudia; Marcuz, Anne; Zenner, Marie-Thérèse; Nettekoven, Matthias H; Ratni, Hasane; Wettstein, Joseph G; Bissantz, Caterina

Malherbe, Pari; Kratzeisen, Claudia; Marcuz, Anne; Zenner, Marie-Thérèse; Nettekoven, Matthias H; Ratni, Hasane; Wettstein, Joseph G; Bissantz, Caterina.

Affiliation

Malherbe P; Discovery Research CNS, F. Hoffmann-La Roche Ltd., PRDN, Building 69/333, CH-4070 Basel, Switzerland. parichehr.malherbe@roche.com

J Med Chem ; 52(22): 7103-12, 2009 Nov 26.

Article in En | MEDLINE | ID: mdl-19817444

Subject(s)

Cell Membrane; Piperidines/chemistry; Piperidines/pharmacology; Receptors, Neurokinin-3/antagonists & inhibitors; Receptors, Neurokinin-3/chemistry; Amino Acid Sequence; Animals; Cattle; Cell Line; Dogs; Guinea Pigs; Humans; Inositol Phosphates/metabolism; Isotope Labeling; Kinetics; Models, Molecular; Molecular Conformation; Molecular Sequence Data; Mutagenesis, Site-Directed; Mutation; Piperidines/metabolism; Protein Structure, Tertiary; Rats; Receptors, Neurokinin-3/genetics; Receptors, Neurokinin-3/metabolism; Reproducibility of Results; Tritium/chemistry

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Cell Membrane / Receptors, Neurokinin-3 Type of study: Diagnostic_studies / Prognostic_studies Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2009 Document type: Article Affiliation country: Switzerland

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