{"doi":"10.1111/cbdd.13743","title":"Novel µ opioid antagonists derived from the µ opioid agonists endomorphin and [Dmt<sup>1</sup>]DALDA (H‐Dmt‐D‐Arg‐Phe‐Lys‐NH<sub>2</sub>)","abstract":"Abstract Hybrid analogues of the µ opioid agonists endomorphin and [Dmt 1 ]DALDA (H‐Dmt‐D‐Arg‐Phe‐Lys‐NH 2 , Dmt = 2′,6′‐dimethyltyrosine) containing cis ‐4‐amino‐Pro, trans ‐4‐amino‐Pro, cis ‐4‐aminoethyl‐Pro or cis ‐4‐guanidinylethyl‐Pro in the 2 position of the peptide sequence were synthesized. None of the compounds retained high µ opioid agonist activity and, unexpectedly, substitution of cis ‐4‐amino‐Pro resulted in a novel class of potent µ opioid antagonists. In particular, the compound H‐Dmt‐ cis ‐4‐amino‐Pro‐Trp‐Lys‐NH 2 (CZ‐1) turned out to be a highly selective µ opioid antagonist with ~1 nM µ receptor binding affinity.","journal":"Chemical Biology & Drug Design","year":2020,"id":116753,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":1,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9488,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":545579,"name":"Jian Xu","orcid":"0000-0003-2032-251X","position":1,"is_corresponding":false},{"id":545580,"name":"Lingling Feng","orcid":"0000-0003-1260-4656","position":2,"is_corresponding":false},{"id":545581,"name":"Xin Fan","orcid":"0009-0006-2398-5043","position":3,"is_corresponding":false},{"id":545582,"name":"Zhen Chen","orcid":"0000-0002-4502-0801","position":4,"is_corresponding":false},{"id":545583,"name":"Yajuan Qin","orcid":"0000-0003-1223-9548","position":5,"is_corresponding":false},{"id":545584,"name":"Nga N. Chung","orcid":"0000-0001-7293-4855","position":6,"is_corresponding":false},{"id":545585,"name":"Tingyou Li","orcid":"0000-0002-4216-2206","position":7,"is_corresponding":false},{"id":545586,"name":"Peter W. Schiller","orcid":"0000-0001-7311-869X","position":8,"is_corresponding":false},{"id":546249,"name":"Saijian Shi","orcid":null,"position":0,"is_corresponding":true}],"reference_count":30,"raw_metadata":null,"created_at":"2026-07-18T23:13:47.803267Z","pmid":"32526055","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}