{"doi":"10.1111/jphp.13317","title":"A CGRP receptor antagonist peptide formulated for nasal administration to treat migraine","abstract":"Abstract Objectives To investigate the formulation of the peptide-based antagonist (34Pro,35Phe)CGRP27–37, of the human calcitonin gene-related peptide (CGRP) receptor as a potential nasally delivered migraine treatment. Methods Peptide sequences were prepared using automated methods and purified by preparative HPLC. Their structure and stability were determined by LC-MS. Antagonist potency was assessed by measuring CGRP-stimulated cAMP accumulation in SK-N-MC, cells and in CHO cells overexpressing the human CGRP receptor. In vivo activity was tested in plasma protein extravasation (PPE) studies using Evans blue dye accumulation. Peptide-containing chitosan microparticles were prepared by spray drying. Key findings (34Pro,35Phe)CGRP27–37 exhibited a 10-fold increased affinity compared to αCGRP27–37. Administration of (34Pro,35Phe)CGRP27–37 to mice led to a significant decrease in CGRP-induced PPE confirming antagonistic properties in vivo. There was no degradation of (34Pro,35Phe)CGRP27–37 and no loss of antagonist potency during formulation and release from chitosan microparticles. Conclusions (34Pro,35Phe)CGRP27–37 is a potent CGRP receptor antagonist both in vitro and in vivo, and it can be formulated as a dry powder with no loss of activity indicating its potential as a nasally formulated anti-migraine medicine.","journal":"Journal of Pharmacy and Pharmacology","year":2020,"id":72920,"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":14,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9519,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"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":273685,"name":"Andrew F. Russo","orcid":"0000-0002-8156-5649","position":1,"is_corresponding":false},{"id":383828,"name":"Zhongming Zhang","orcid":"0000-0002-6289-2353","position":2,"is_corresponding":false},{"id":383829,"name":"Adisa Kuburas","orcid":"0009-0000-1121-7932","position":3,"is_corresponding":false},{"id":383830,"name":"Patrick M. Killoran","orcid":"0000-0001-7294-405X","position":4,"is_corresponding":false},{"id":383831,"name":"Vera D’Aloisio","orcid":"0000-0003-3377-4283","position":5,"is_corresponding":false},{"id":384548,"name":"Laura Nižić","orcid":null,"position":6,"is_corresponding":false},{"id":384549,"name":"Vicky Capel","orcid":null,"position":7,"is_corresponding":false},{"id":383832,"name":"David A. Kendall","orcid":"0000-0001-8740-6764","position":8,"is_corresponding":false},{"id":383833,"name":"Christopher R. Coxon","orcid":"0000-0002-3375-3901","position":9,"is_corresponding":false},{"id":383834,"name":"Gillian A. Hutcheon","orcid":"0000-0002-9786-2074","position":10,"is_corresponding":false},{"id":384547,"name":"Bengt von Mentzer","orcid":null,"position":0,"is_corresponding":true}],"reference_count":33,"raw_metadata":null,"created_at":"2026-07-18T21:45:09.279825Z","pmid":"32588458","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":[]}