Recent advances in neurokinin receptor antagonists.
The structurally related neuropeptides, substance P (SP), neurokinin A (NKA), and neurokinin B (NKB), which belong to a family of molecules termed tachykinins and are widely distributed in the central and peripheral nervous systems, influence the function of many tissues. SP and NKA have links to the following chronic diseases: asthma, inflammatory bowel disorders, rheumatoid arthritis, pain and psychiatric disorders. These peptides exert their effects through three G-protein coupled receptor subtypes, namely, the NK1, NK2, and NK3 receptors. Non-peptide antagonists of these receptors may provide opportunities for disease treatments. In this review, the very recent advances in nonpeptide neurokinin receptor antagonists will be described with an emphasis on structure-activity relationships which have been developed.
Gao
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Hoechst Marion Roussel, Inc., Medicinal Chemistry, Route 202-206 North, Bridgewater, NJ 08807, USA.
Peet
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D000595:Amino Acid Sequence; D000818:Animals; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D018042:Receptors, Neurokinin-3 / Q000037:antagonists & inhibitors*
D018041:Receptors, Neurokinin-2; D018042:Receptors, Neurokinin-3