期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 4, 期 1, 页码 1-17出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026043451618
关键词
opioid peptides; opioid agonists and antagonists; structure-activity relationships; opioid receptor selectivity; receptor binding assay
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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