{"doi":"10.1016/s0014-2999(98)00975-3","title":"Novel potent AMPA analogues differentially affect desensitisation of AMPA receptors in cultured hippocampal neurons","abstract":null,"journal":"European Journal of Pharmacology","year":1999,"id":623099,"datarank":0.26876392038420827,"base_score":1.791759469228055,"endowment":1.791759469228055,"self_citation_contribution":0.26876392038420827,"citation_network_contribution":0.0,"self_endowment_contribution":0.26876392038420827,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":5,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1610244,"name":"John D.C Lambert","orcid":null,"position":1,"is_corresponding":false},{"id":1610243,"name":"Tue G Banke","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Novel potent AMPA analogues differentially affect desensitisation of AMPA receptors in cultured hippocampal neurons","abstract":"The agonist actions of two AMPA receptor analogues, (RS)-2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and (RS)-2-amino-3-(3-hydroxy-5-trfluoromethyl-4-isoxazolyl)prop ionic acid (Tri-F-AMPA) have been studied on cultured rat hippocampal neurons. Whole-cell recordings with semi-rapid application of the agonists were used to study steady-state (plateau) responses. ACPA was the most potent agonist (EC50, 1.2 microM), followed by AMPA (4.3 microM) and Tri-F-AMPA (4.6 microM), corresponding to a potency ratio of 4:1:1. Hill coefficients were close to 1 for AMPA and ACPA and close to 2 for Tri-F-AMPA, respectively. Plateau responses to maximal concentrations of the three agonists varied more than 2-fold. ACPA responses were 2.1 times greater and responses to Tri-F-AMPA were 1.6 times greater than responses to AMPA, respectively. Peak responses and desensitization were studied by using a fast piezoelectric device to apply agonists rapidly to outside-out patches. The time constants of desensitization were 8 ms for AMPA, 12 ms for Tri-F-AMPA and 17 ms for ACPA. There were no significant differences in the time-to-peak and 10-90% rise-time of the responses. The results indicate that of the three agonists tested, ACPA is the most potent at AMPA receptors expressed in cultured hippocampal neurons and that the maximum response to the agonists is inversely related to the rate of desensitization.","is_dataset_classified":null,"base_score":1.6094379124341003,"endowment":1.6094379124341003,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"10079017","pmcid":null,"openalex_id":"https://openalex.org/W2068533370","authors":[],"funders":[],"total_grants":0,"fwci":0.4246,"citation_percentile":0.50694399,"influential_citations":0,"citation_trend":[],"oa_status":"closed","license":"https://www.elsevier.com/tdm/userlicense/1.0/","oa_locations":[{"url":"https://api.elsevier.com/content/article/PII:S0014299998009753?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0014299998009753?httpAccept=text/plain","host_type":"publisher"},{"url":"https://doi.org/10.1016/s0014-2999(98)00975-3","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/10079017","host_type":"repository"},{"url":"https://pure.au.dk/portal/en/publications/06f84c35-1ce0-468a-8bc5-49fc01f0dd6b","host_type":""}],"fields_of_study":["Neuroscience and Neuropharmacology Research","Receptor Mechanisms and Signaling","Lipid Membrane Structure and Behavior","Cells, Cultured","Hippocampus","Humans","Neurons","Receptors, AMPA","Time Factors","alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid"],"mesh_terms":["Cells, Cultured","Hippocampus","Humans","Neurons","Time Factors","Receptors, AMPA","alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid"],"keywords":["AMPA receptor","Agonist","Desensitization (medicine)","Glutamate receptor","Hippocampal formation","Chemistry","Receptor","Neuroscience","Endocrinology","Internal medicine","Biology","Biochemistry","Medicine"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-03T22:23:40.125680Z","pmid":null,"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":[]}