Replacement of the quinoline system in 2-phenyl-4-quinolinecarboxamide NK-3 receptor antagonists

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Yung-Chi Cheng, William H. Prusoff · Biochemical Pharmacology · 1973 · 12.9K citations

Life Sciences, Biochemistry, Chemical Kinetics +14

SR 142801, The first potent non-peptide antagonist of the tachykinin NK3 receptor

Xavier Emonds‐Alt, Daniel Bichon, Jean-Philippe Ducoux et al. · Life Sciences · 1994 · 219 citations · Full text

Medicine, Pharmacology, Molecular Pharmacology +3

Molecular characterisation, expression and localisation of human neurokinin‐3 receptor

Gary Buell, Matthias Schulz, S. J. Arkinstall et al. · FEBS Letters · 1992 · 115 citations · Full text

Life Sciences, Molecular Biology, Neuroscience +16

Nonpeptide Tachykinin Receptor Antagonists: I. Pharmacological and Pharmacokinetic Characterization of SB 223412, a Novel, Potent and Selective Neurokinin-3 Receptor Antagonist

Henry M. Sarau, Don E. Griswold, W. M. Potts et al. · Journal of Pharmacology and Experimental Therapeutics · 1997 · 107 citations · Full text

Medicine, Pharmacokinetics, Pharmacology +10

Discovery of a Novel Class of Selective Non-Peptide Antagonists for the Human Neurokinin-3 Receptor. 1. Identification of the 4-Quinolinecarboxamide Framework

Giuseppe Giardina, Henry M. Sarau, Carlo Farina et al. · Journal of Medicinal Chemistry · 1997 · 79 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +12