1131739-62-2Relevant academic research and scientific papers
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
supporting information; experimental part, p. 7103 - 7112 (2010/06/12)
In this study, we show that compound 3 (osanetant) binds with a pseudoirreversible, apparent noncompetitive mode of antagonism at the guinea pig NK3, while it behaves competitively at the human NK3. This difference is caused by a slo
PIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS
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Page/Page column 13, (2009/04/24)
The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5′ or to a pharmaceutically active salt thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
