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• W2110366466 endingPage "410" @default.
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• W2110366466 abstract "The discovery of endogenous opioid peptides 25 years ago opened up a new chapter in efforts to understand the origins and control of pain, its relationships to other biological functions, including inflammatory and other immune responses, and the relationships of opioid peptides and their receptors to a variety of undesirable or toxic side effects often associated with the nonpeptide opiates such as morphine including addiction, constipation, a variety of neural toxicities, tolerance, and respiratory depression. For these investigations the need for potent and highly receptor selective agonists and antagonists has been crucial since they in principle allow one to distinguish unequivocally the roles of the different opioid receptors (μ, δ, and κ) in the various biological and pathological roles of the opioid peptides and their receptors. Conformational and topographical constraint of the linear natural endogenous opioid peptides has played a major role in developing peptide ligands with high selectivity for μ, δ, and κ receptors, and in understanding the conformational, topographical, and stereoelectronic structural requirements of the opioid peptides for their interactions with opioid receptors. In turn, this had led to insights into the three-dimensional pharmacophore for opioid receptors. In this article we review and discuss some of the developments that have led to potent, selective, and stable peptide and peptidomimetic ligands that are highly potent and selective, and that have δ agonist, μ antagonist, and κ agonist biological activities (other authors in this issue will discuss the development of other types of activities and selectivities). These have led to ligands that provide unique insight into opioid pharmacophores and the critical roles opioid ligands and receptor scan play in pain, addiction, and other human maladies. © 2000 John Wiley & Sons, Inc. Biopoly 51: 391–410, 1999" @default.
• W2110366466 created "2016-06-24" @default.
• W2110366466 creator A5026107561 @default.
• W2110366466 creator A5076760321 @default.
• W2110366466 date "1999-01-01" @default.
• W2110366466 modified "2023-10-04" @default.
• W2110366466 title "Conformation-activity relationships of opioid peptides with selective activities at opioid receptors" @default.
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• W2110366466 doi "https://doi.org/10.1002/(sici)1097-0282(1999)51:6<391::aid-bip3>3.0.co;2-x" @default.
• W2110366466 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10797229" @default.
• W2110366466 hasPublicationYear "1999" @default.
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