Abstract
MEN 15596 is a small molecule, potent and selective antagonist of NK(2) receptor, possessing high affinity and potency at the guinea-pig and human receptors whose pharmacological characterization has been recently published. Here we report how the corresponding class of compounds was derived from a tri-peptide library and the first optimization round to improve both in vitro activity and physicochemical properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acids / chemistry*
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Animals
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Chemistry, Pharmaceutical / methods
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Drug Design
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Guinea Pigs
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Humans
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Hydrogen-Ion Concentration
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Kinetics
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Models, Chemical
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Models, Molecular
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Molecular Conformation
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Peptides / chemistry
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Phenylalanine / chemistry
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Receptors, Neurokinin-2 / antagonists & inhibitors*
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Solubility
Substances
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Amino Acids
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Peptides
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Receptors, Neurokinin-2
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Phenylalanine