{"id":"https://openalex.org/W12842836","doi":null,"title":"Potent and use-dependent block of cardiac sodium channels by U-50,488H, a benzeneacetamide kappa opioid receptor agonist.","display_name":"Potent and use-dependent block of cardiac sodium channels by U-50,488H, a benzeneacetamide kappa opioid receptor agonist.","publication_year":2001,"publication_date":"2001-01-01","ids":{"openalex":"https://openalex.org/W12842836","mag":"12842836","pmid":"https://pubmed.ncbi.nlm.nih.gov/20428265","pmcid":"https://www.ncbi.nlm.nih.gov/pmc/articles/2859007"},"language":"en","primary_location":{"id":"pmh:oai:pubmedcentral.nih.gov:2859007","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/2859007","pdf_url":null,"source":{"id":"https://openalex.org/S2764455111","display_name":"PubMed Central","issn_l":null,"issn":null,"is_oa":true,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Exp Clin Cardiol","raw_type":"Text"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["pubmed"],"open_access":{"is_oa":true,"oa_status":"green","oa_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/2859007","any_repository_has_fulltext":true},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5081274926","display_name":"Michael K. Pugsley","orcid":"https://orcid.org/0000-0002-4626-9975","observed_orcids":["https://orcid.org/0000-0002-4626-9975"]},"institutions":[{"id":"https://openalex.org/I204250578","display_name":"University of California, Irvine","ror":"https://ror.org/04gyf1771","country_code":"US","type":"education","lineage":["https://openalex.org/I204250578"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"M K Pugsley","raw_affiliation_strings":["Department of Microbiology & Molecular Genetics, University of California, Irvine, California, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Microbiology & Molecular Genetics, University of California, Irvine, California, USA","institution_ids":["https://openalex.org/I204250578"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5082951686","display_name":"Esther J. Yu","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"E J Yu","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5003520814","display_name":"Alan L. Goldin","orcid":"https://orcid.org/0000-0001-7159-0288","observed_orcids":["https://orcid.org/0000-0001-7159-0288"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"A L Goldin","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":0.4555,"has_fulltext":false,"cited_by_count":5,"citation_normalized_percentile":{"value":0.68034965,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":96},"biblio":{"volume":"6","issue":"2","first_page":"61","last_page":"71"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10217","display_name":"Cardiac electrophysiology and arrhythmias","score":0.5605000257492065,"subfield":{"id":"https://openalex.org/subfields/2705","display_name":"Cardiology and Cardiovascular Medicine"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T10217","display_name":"Cardiac electrophysiology and arrhythmias","score":0.5605000257492065,"subfield":{"id":"https://openalex.org/subfields/2705","display_name":"Cardiology and Cardiovascular Medicine"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T10493","display_name":"Ion channel regulation and function","score":0.4311999976634979,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10814","display_name":"Neuropeptides and Animal Physiology","score":0.0017999999690800905,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/u50-488h","display_name":"U50,488H","score":0.996999979019165},{"id":"https://openalex.org/keywords/kappa-opioid-receptor-agonists","display_name":"kappa opioid receptor agonists","score":0.949999988079071},{"id":"https://openalex.org/keywords/use-dependent-block","display_name":"use-dependent block","score":0.9599999785423279},{"id":"https://openalex.org/keywords/lidocaine","display_name":"lidocaine","score":0.8209999799728394},{"id":"https://openalex.org/keywords/sodium-current","display_name":"sodium current","score":0.7110000252723694},{"id":"https://openalex.org/keywords/antiarrhythmic-drugs","display_name":"antiarrhythmic drugs","score":0.8920000195503235},{"id":"https://openalex.org/keywords/arylacetamides","display_name":"arylacetamides","score":0.7649999856948853},{"id":"https://openalex.org/keywords/channel-inactivation","display_name":"channel inactivation","score":0.527999997138977},{"id":"https://openalex.org/keywords/recovery-from-inactivation","display_name":"recovery from inactivation","score":0.7799999713897705},{"id":"https://openalex.org/keywords/molecular-probes","display_name":"molecular probes","score":0.38499999046325684}],"concepts":[{"id":"https://openalex.org/C50952357","wikidata":"https://www.wikidata.org/wiki/Q424960","display_name":"Sodium channel","level":3,"score":0.9028074741363525},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.5840084552764893},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.5799550414085388},{"id":"https://openalex.org/C2776414672","wikidata":"https://www.wikidata.org/wiki/Q7553303","display_name":"Sodium channel blocker","level":4,"score":0.5418643951416016},{"id":"https://openalex.org/C79743260","wikidata":"https://www.wikidata.org/wiki/Q2882301","display_name":"Cardiac action potential","level":4,"score":0.5394424200057983},{"id":"https://openalex.org/C4141045","wikidata":"https://www.wikidata.org/wiki/Q83183","display_name":"Depolarization","level":2,"score":0.49764493107795715},{"id":"https://openalex.org/C2777561782","wikidata":"https://www.wikidata.org/wiki/Q420377","display_name":"Mexiletine","level":2,"score":0.4827632009983063},{"id":"https://openalex.org/C12554922","wikidata":"https://www.wikidata.org/wiki/Q7100","display_name":"Biophysics","level":1,"score":0.4417421519756317},{"id":"https://openalex.org/C50254741","wikidata":"https://www.wikidata.org/wiki/Q62536","display_name":"Ion channel","level":3,"score":0.42704105377197266},{"id":"https://openalex.org/C537181965","wikidata":"https://www.wikidata.org/wiki/Q658","display_name":"Sodium","level":2,"score":0.3728938102722168},{"id":"https://openalex.org/C42219234","wikidata":"https://www.wikidata.org/wiki/Q131130","display_name":"Anesthesia","level":1,"score":0.3343650698661804},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.3232104778289795},{"id":"https://openalex.org/C185263204","wikidata":"https://www.wikidata.org/wiki/Q1154774","display_name":"Electrophysiology","level":2,"score":0.3169187903404236},{"id":"https://openalex.org/C126322002","wikidata":"https://www.wikidata.org/wiki/Q11180","display_name":"Internal medicine","level":1,"score":0.2543941140174866},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.24740207195281982},{"id":"https://openalex.org/C146403970","wikidata":"https://www.wikidata.org/wiki/Q205729","display_name":"Repolarization","level":3,"score":0.2204553484916687},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.1420479118824005},{"id":"https://openalex.org/C178790620","wikidata":"https://www.wikidata.org/wiki/Q11351","display_name":"Organic chemistry","level":1,"score":0.0}],"mesh":[],"locations_count":3,"locations":[{"id":"pmh:oai:pubmedcentral.nih.gov:2859007","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/2859007","pdf_url":null,"source":{"id":"https://openalex.org/S2764455111","display_name":"PubMed Central","issn_l":null,"issn":null,"is_oa":true,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Exp Clin Cardiol","raw_type":"Text"},{"id":"pmid:20428265","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/20428265","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Experimental and clinical cardiology","raw_type":"Journal Article"},{"id":"mag:12842836","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/20428265","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":"PubMed","raw_type":null}],"best_oa_location":{"id":"pmh:oai:pubmedcentral.nih.gov:2859007","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/2859007","pdf_url":null,"source":{"id":"https://openalex.org/S2764455111","display_name":"PubMed Central","issn_l":null,"issn":null,"is_oa":true,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Exp Clin Cardiol","raw_type":"Text"},"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.8371999859809875}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":36,"referenced_works":["https://openalex.org/W1231310421","https://openalex.org/W1765976842","https://openalex.org/W1952388191","https://openalex.org/W1963515358","https://openalex.org/W1966818330","https://openalex.org/W1970599367","https://openalex.org/W1972523062","https://openalex.org/W1973235666","https://openalex.org/W1975459135","https://openalex.org/W1976219194","https://openalex.org/W1981271402","https://openalex.org/W1985146688","https://openalex.org/W1985940938","https://openalex.org/W1986440044","https://openalex.org/W1993584057","https://openalex.org/W1998151458","https://openalex.org/W2007164935","https://openalex.org/W2014953544","https://openalex.org/W2036295857","https://openalex.org/W2042185302","https://openalex.org/W2056469720","https://openalex.org/W2069884282","https://openalex.org/W2069899558","https://openalex.org/W2079604571","https://openalex.org/W2114605607","https://openalex.org/W2115052737","https://openalex.org/W2116411564","https://openalex.org/W2120744579","https://openalex.org/W2125875893","https://openalex.org/W2145099840","https://openalex.org/W2167852072","https://openalex.org/W2168564324","https://openalex.org/W2173730295","https://openalex.org/W2270573307","https://openalex.org/W2337691965","https://openalex.org/W2464059395"],"related_works":["https://openalex.org/W1972523062","https://openalex.org/W317370711","https://openalex.org/W1963515358","https://openalex.org/W2278694116","https://openalex.org/W2050987297","https://openalex.org/W2214114766","https://openalex.org/W2028890503","https://openalex.org/W1985059368","https://openalex.org/W2356296907","https://openalex.org/W2383132758"],"abstract_inverted_index":{"OBJECTIVES:":[0],"To":[1],"determine":[2],"whether":[3],"the":[4,14,25,103,170,183,206],"kappa":[5],"opioid":[6],"receptor":[7],"agonist":[8],"U-50,488H,":[9],"a":[10,19,52,80,99,124,133,165,200],"benzacetamide":[11],"derivative":[12],"of":[13,28,31,44,50,84,106,136,148,158,174,185],"cyclo-hexane-1,2-diamine":[15],"analgesics,":[16],"may":[17,161,178],"be":[18],"useful":[20],"molecular":[21],"probe":[22],"to":[23,168],"define":[24],"structural":[26,156,176],"requirements":[27],"this":[29,159],"class":[30,55],"drugs":[32,97,117,189],"for":[33],"cardiac":[34,149],"sodium":[35,62,85,107,150],"channel":[36,108,196],"blockade.":[37],"ANIMALS":[38],"AND":[39],"METHODS:":[40],"The":[41,141],"electrophysiological":[42],"effects":[43],"U-50,488H":[45,76,88,122,153],"were":[46],"compared":[47,129],"with":[48,130,164],"those":[49],"lidocaine,":[51],"clinically":[53],"used":[54],"Ib":[56],"antiarrhythmic":[57,188,203],"agent,":[58],"in":[59,65,102,127,182,199,205],"rat":[60],"heart":[61],"currents":[63],"expressed":[64],"Xenopus":[66],"laevis":[67],"oocytes":[68],"by":[69,152],"using":[70],"two-electrode":[71],"voltage":[72,104],"clamp.":[73],"RESULTS:":[74],"Both":[75,96,116],"and":[77,110,145,190],"lidocaine":[78,131],"produced":[79,98],"concentration-dependent":[81],"tonic":[82,144],"block":[83,147,169],"current,":[86],"but":[87,121],"was":[89],"approximately":[90],"fourfold":[91],"more":[92,142],"potent":[93,143],"than":[94],"lidocaine.":[95],"hyperpolarizing":[100],"shift":[101],"dependence":[105],"inactivation":[109],"both":[111],"delayed":[112],"recovery":[113],"from":[114],"inactivation.":[115],"exhibited":[118],"use-dependent":[119,146],"block,":[120,197],"showed":[123],"1.8-fold":[125],"increase":[126],"potency":[128],"at":[132],"high":[134],"frequency":[135],"stimulation":[137],"(30":[138],"Hz).":[139],"CONCLUSIONS:":[140],"channels":[151],"suggests":[154],"that":[155],"features":[157,177],"molecule":[160],"provide":[162,179],"it":[163],"greater":[166],"ability":[167],"channel.":[171],"An":[172],"understanding":[173],"these":[175],"information":[180],"needed":[181],"development":[184],"novel":[186],"arylacetamide-based":[187],"insight":[191],"into":[192],"possible":[193],"mechanisms":[194],"describing":[195],"resulting":[198],"highly":[201],"efficacious":[202],"action":[204],"heart.":[207]},"counts_by_year":[{"year":2024,"cited_by_count":1},{"year":2016,"cited_by_count":2}],"updated_date":"2026-10-28T10:33:24.094632","created_date":"2016-06-24T00:00:00"}
