4.4 Review

Opioid receptors and their ligands

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CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 4, 期 1, 页码 1-17

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BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026043451618

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opioid peptides; opioid agonists and antagonists; structure-activity relationships; opioid receptor selectivity; receptor binding assay

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This review gives a historical perspective, summarizing approximately 25 years of research on opioids. The typical opioid peptides produced in the brain, atypical opioids encrypted in milk protein or hemoglobin sequences, and extremely potent and selective opioids of amphibian origin are described. The main focus is on the structure-activity relationship studies of peptide ligands for three main opioid receptor types (mu, delta, kappa), their selectivities and pharmacological activities in vitro. Chemical modifications that led to obtaining potent and selective agonists and antagonists for these receptors are discussed.

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