Biochemical and Biophysical Research Communications
Regular ArticleIdentification of Methionine 134 and Alanine 146 in the Second Transmembrane Segment of the Human Tachykinin NK3 Receptor as Residues Involved in Species-Selective Binding to SR 48968
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Mapping the binding pocket of a novel, high-affinity, slow dissociating tachykinin NK<inf>3</inf> receptor antagonist: Biochemical and electrophysiological characterization
2014, NeuropharmacologyCitation Excerpt :Osanetant was then manually docked into the transmembrane cavity of the hNK3 model. The docking mode was based on the following hypotheses: 1) the ligand should make a direct interaction with Met1342.53 since this residue has been shown to be responsible for species selectivity of N-[(S)-4-(4-Acetylamino-4-phenyl-piperidin-1-yl)-2-(3,4-dichloro-phenyl)-butyl]-N-methyl-benzamide (saredutant, SR 48968) (Wu et al., 1994). 2) Phenyl-piperidine substructures are privileged fragments for the subpocket formed by the transmembrane domains 3, 5 and 6.
Acute nicotine and phencyclidine increase locomotor activity of the guinea pig with attenuated potencies relative to their effects on rat or mouse
2010, Pharmacology Biochemistry and BehaviorCharacterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3
2009, Biochemical PharmacologyCitation Excerpt :Compounds from different structural classes have 5–10-fold lower potency and 10–50-fold lower affinity for rodent NK3R compared to human counterparts [20,21]. Site-directed mutagenesis studies indicate that two AA in the second transmembrane domain of the human NK3R (Met134 and Ala146) were responsible for these species differences [20,22]. However, as is the case for NK2R, the identity of NK3R from dog and gerbil remain unknown.
Molecular and pharmacological characterization of the murine tachykinin NK<inf>3</inf> receptor
2001, European Journal of PharmacologyBacterial expression and characterization of human recombinant apolipoprotein(a) kringle IV type 9
1998, Protein Expression and Purification