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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Non-peptide Opioid Receptor Ligands - Recent Advances. Part II - Antagonists

Author(s): Agnieszka Kaczor and Dariusz Matosiuk

Volume 9 , Issue 17 , 2002

Page: [1591 - 1603] Pages: 13

DOI: 10.2174/0929867023369358

Price: $65


This paper is the second part of the review on opioid receptor ligands and deals with the progress in the field of non-peptide opioid receptor antagonists (starting from the pioneering opiate studies in the early seventies) with particular stress on the last decade accomplishments. As X-ray high resolution structure determination of the ligand-receptor systems for G protein-coupled receptors meets with considerable experimental obstacles, the knowledge about ligand interactions with the membrane-bound receptors traditionally derives from structure-activity studies. Hence, such a concise summary, collecting chemically distinct but pharmalogically relative compounds, may be a convenient information source for any research concerning ligand-opioid receptor binding or rational drug design.

Keywords: non-peptide opioid receptor, norbinaltorphimine derived ligands, de novo methodology, pharmacophore models, pyrrolomorphinans, kappa opioid receptor

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