{"id":"https://openalex.org/W1988345751","doi":"https://doi.org/10.1111/j.1432-1033.1982.tb06658.x","title":"Agonist\u2010Mediated Conformational Changes of Muscarinic Receptors in Rat Brain","display_name":"Agonist\u2010Mediated Conformational Changes of Muscarinic Receptors in Rat Brain","publication_year":1982,"publication_date":"1982-06-01","ids":{"openalex":"https://openalex.org/W1988345751","doi":"https://doi.org/10.1111/j.1432-1033.1982.tb06658.x","mag":"1988345751","pmid":"https://pubmed.ncbi.nlm.nih.gov/7106116"},"language":"en","primary_location":{"id":"doi:10.1111/j.1432-1033.1982.tb06658.x","doi":"https://doi.org/10.1111/j.1432-1033.1982.tb06658.x","is_oa":false,"landing_page_url":"https://doi.org/10.1111/j.1432-1033.1982.tb06658.x","pdf_url":null,"source":{"id":"https://openalex.org/S4210214924","display_name":"European Journal of Biochemistry","issn_l":"0014-2956","issn":["0014-2956","0945-5795","1432-1033"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","poland-100"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"European Journal of Biochemistry","raw_type":"journal-article"},"volume":null,"type":"article","indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5065113357","display_name":"Georges Vauquelin","orcid":"https://orcid.org/0000-0001-8613-1711","observed_orcids":["https://orcid.org/0000-0001-8613-1711"]},"institutions":[{"id":"https://openalex.org/I13469542","display_name":"Vrije Universiteit Brussel","ror":"https://ror.org/006e5kg04","country_code":"BE","type":"education","lineage":["https://openalex.org/I13469542"]}],"countries":["BE"],"is_corresponding":true,"raw_author_name":"Georges VAUQUELIN","raw_affiliation_strings":["Laboratorium voor Pathologische Biochemie, Instituut voor Moleculaire Biologie, Vrije Universiteit (te) Brussel, Paardestraat 65, B-1640 Sint-Genesius-Rode, Belgium"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratorium voor Pathologische Biochemie, Instituut voor Moleculaire Biologie, Vrije Universiteit (te) Brussel, Paardestraat 65, B-1640 Sint-Genesius-Rode, Belgium","institution_ids":["https://openalex.org/I13469542"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5103411812","display_name":"Claudine Andr\u00e9","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I13469542","display_name":"Vrije Universiteit Brussel","ror":"https://ror.org/006e5kg04","country_code":"BE","type":"education","lineage":["https://openalex.org/I13469542"]}],"countries":["BE"],"is_corresponding":false,"raw_author_name":"Claudine ANDR\u00c9","raw_affiliation_strings":["Laboratorium voor Pathologische Biochemie, Instituut voor Moleculaire Biologie, Vrije Universiteit (te) Brussel, Paardestraat 65, B-1640 Sint-Genesius-Rode, Belgium"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratorium voor Pathologische Biochemie, Instituut voor Moleculaire Biologie, Vrije Universiteit (te) Brussel, Paardestraat 65, B-1640 Sint-Genesius-Rode, Belgium","institution_ids":["https://openalex.org/I13469542"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5084009630","display_name":"Jean\u2010Paul De Backer","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I13469542","display_name":"Vrije Universiteit Brussel","ror":"https://ror.org/006e5kg04","country_code":"BE","type":"education","lineage":["https://openalex.org/I13469542"]}],"countries":["BE"],"is_corresponding":false,"raw_author_name":"Jean\u2010Paul DE BACKER","raw_affiliation_strings":["Laboratorium voor Pathologische Biochemie, Instituut voor Moleculaire Biologie, Vrije Universiteit (te) Brussel, Paardestraat 65, B-1640 Sint-Genesius-Rode, Belgium"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratorium voor Pathologische Biochemie, Instituut voor Moleculaire Biologie, Vrije Universiteit (te) Brussel, Paardestraat 65, B-1640 Sint-Genesius-Rode, Belgium","institution_ids":["https://openalex.org/I13469542"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111789668","display_name":"Pierre M. Laduron","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I137982388","display_name":"Janssen (Belgium)","ror":"https://ror.org/04yzcpd71","country_code":"BE","type":"company","lineage":["https://openalex.org/I1330063522","https://openalex.org/I137982388"]}],"countries":["BE"],"is_corresponding":false,"raw_author_name":"Pierre LADURON","raw_affiliation_strings":["De\u0301partement de Pharmacologie Biochimique, Janssen Pharmaceutica, B-2340 Beerse, Belgium","D\u00e9partement de Pharmacologie Biochimique, Janssen Pharmaceutica, B-2340 Beerse, Belgium"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"De\u0301partement de Pharmacologie Biochimique, Janssen Pharmaceutica, B-2340 Beerse, Belgium","institution_ids":["https://openalex.org/I137982388"]},{"raw_affiliation_string":"D\u00e9partement de Pharmacologie Biochimique, Janssen Pharmaceutica, B-2340 Beerse, Belgium","institution_ids":["https://openalex.org/I137982388"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5113837546","display_name":"Arthur Donny Strosberg","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1294671590","display_name":"Centre National de la Recherche Scientifique","ror":"https://ror.org/02feahw73","country_code":"FR","type":"government","lineage":["https://openalex.org/I1294671590"]},{"id":"https://openalex.org/I4387154366","display_name":"Universit\u00e9 Paris Diderot","ror":"https://ror.org/02n7qrg46","country_code":"FR","type":"education","lineage":["https://openalex.org/I204730241","https://openalex.org/I4387154366"]}],"countries":["FR"],"is_corresponding":false,"raw_author_name":"A. Donny STROSBERG","raw_affiliation_strings":["Laboratoire d'lmmunologie Mole\u0301culaire, Institut de Recherche en Biologie Mole\u0301culaire du Centre National de la Recherche Scientifique, Universite de Paris VII, Tour 43, 2 Place Jussieu, F-75 221 Paris-Cedex-05, France","Laboratoire d'lmmunologie Mol\u00e9culaire, Institut de Recherche en Biologie Mol\u00e9culaire du Centre National de la Recherche Scientifique, Universite de Paris VII, Tour 43, 2 Place Jussieu, F\u201075 221 Paris\u2010Cedex\u201005, France"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratoire d'lmmunologie Mole\u0301culaire, Institut de Recherche en Biologie Mole\u0301culaire du Centre National de la Recherche Scientifique, Universite de Paris VII, Tour 43, 2 Place Jussieu, F-75 221 Paris-Cedex-05, France","institution_ids":["https://openalex.org/I1294671590","https://openalex.org/I4387154366"]},{"raw_affiliation_string":"Laboratoire d'lmmunologie Mol\u00e9culaire, Institut de Recherche en Biologie Mol\u00e9culaire du Centre National de la Recherche Scientifique, Universite de Paris VII, Tour 43, 2 Place Jussieu, F\u201075 221 Paris\u2010Cedex\u201005, France","institution_ids":["https://openalex.org/I1294671590","https://openalex.org/I4387154366"]}]}],"institutions":[],"countries_distinct_count":2,"institutions_distinct_count":4,"corresponding_author_ids":["https://openalex.org/A5065113357"],"corresponding_institution_ids":["https://openalex.org/I13469542"],"apc_list":null,"apc_paid":null,"fwci":2.7206,"has_fulltext":false,"cited_by_count":26,"citation_normalized_percentile":{"value":0.90705248,"is_in_top_1_percent":false,"is_in_top_10_percent":true},"cited_by_percentile_year":null,"biblio":{"volume":"125","issue":"1","first_page":"117","last_page":"124"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.9990000128746033,"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"}},"topics":[{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.9990000128746033,"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/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.0006000000284984708,"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"}},{"id":"https://openalex.org/T11818","display_name":"Nicotinic Acetylcholine Receptors Study","score":0.00019999999494757503,"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"}}],"keywords":[{"id":"https://openalex.org/keywords/muscarinic-receptors","display_name":"muscarinic receptors","score":0.9959999918937683},{"id":"https://openalex.org/keywords/receptor-conformational-change","display_name":"receptor conformational change","score":0.7870000004768372},{"id":"https://openalex.org/keywords/n-ethylmaleimide-alkylation","display_name":"N-ethylmaleimide alkylation","score":0.8949999809265137},{"id":"https://openalex.org/keywords/carbachol","display_name":"carbachol","score":0.7860000133514404},{"id":"https://openalex.org/keywords/receptor-subpopulations","display_name":"receptor subpopulations","score":0.8169999718666077},{"id":"https://openalex.org/keywords/agonist-binding-affinity","display_name":"agonist affinity","score":0.7760000228881836},{"id":"https://openalex.org/keywords/monod-wyman-changeux-model","display_name":"Monod-Wyman-Changeux model","score":0.8360000252723694},{"id":"https://openalex.org/keywords/active-conformation","display_name":"active conformation","score":0.5429999828338623},{"id":"https://openalex.org/keywords/rat-forebrain","display_name":"rat forebrain","score":0.5920000076293945}],"concepts":[{"id":"https://openalex.org/C2778938600","wikidata":"https://www.wikidata.org/wiki/Q389934","display_name":"Agonist","level":3,"score":0.7425440549850464},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.726235032081604},{"id":"https://openalex.org/C33789571","wikidata":"https://www.wikidata.org/wiki/Q410959","display_name":"Muscarinic acetylcholine receptor","level":3,"score":0.667894184589386},{"id":"https://openalex.org/C86811712","wikidata":"https://www.wikidata.org/wiki/Q410943","display_name":"Competitive antagonist","level":4,"score":0.5617377161979675},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.5612098574638367},{"id":"https://openalex.org/C107824862","wikidata":"https://www.wikidata.org/wiki/Q616005","display_name":"Binding site","level":2,"score":0.4937470853328705},{"id":"https://openalex.org/C2777646807","wikidata":"https://www.wikidata.org/wiki/Q292393","display_name":"N-Ethylmaleimide","level":2,"score":0.4376934766769409},{"id":"https://openalex.org/C74998103","wikidata":"https://www.wikidata.org/wiki/Q898254","display_name":"Dissociation constant","level":3,"score":0.4209998548030853},{"id":"https://openalex.org/C12554922","wikidata":"https://www.wikidata.org/wiki/Q7100","display_name":"Biophysics","level":1,"score":0.33947810530662537},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.32188475131988525},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3081953227519989},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.15781277418136597}],"mesh":[{"descriptor_ui":"D000477","descriptor_name":"Alkylating Agents","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001667","descriptor_name":"Binding, Competitive","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001923","descriptor_name":"Brain Chemistry","qualifier_ui":null,"qualifier_name":null,"is_major_topic":true},{"descriptor_ui":"D003909","descriptor_name":"Dexetimide","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D005033","descriptor_name":"Ethylmaleimide","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D008297","descriptor_name":"Male","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D010277","descriptor_name":"Parasympathomimetics","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D011487","descriptor_name":"Protein Conformation","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011919","descriptor_name":"Rats, Inbred Strains","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011950","descriptor_name":"Receptors, Cholinergic","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D011976","descriptor_name":"Receptors, Muscarinic","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D051381","descriptor_name":"Rats","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1111/j.1432-1033.1982.tb06658.x","doi":"https://doi.org/10.1111/j.1432-1033.1982.tb06658.x","is_oa":false,"landing_page_url":"https://doi.org/10.1111/j.1432-1033.1982.tb06658.x","pdf_url":null,"source":{"id":"https://openalex.org/S4210214924","display_name":"European Journal of Biochemistry","issn_l":"0014-2956","issn":["0014-2956","0945-5795","1432-1033"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","poland-100"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"European Journal of Biochemistry","raw_type":"journal-article"},{"id":"pmid:7106116","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/7106116","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":"European journal of biochemistry","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"score":0.4000000059604645,"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3"}],"sustainable_development_goals_aurora":[],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":36,"referenced_works":["https://openalex.org/W278096561","https://openalex.org/W1585579824","https://openalex.org/W1775749144","https://openalex.org/W1855289338","https://openalex.org/W1965681249","https://openalex.org/W1967393911","https://openalex.org/W1996152329","https://openalex.org/W1998093640","https://openalex.org/W1999153149","https://openalex.org/W2001668716","https://openalex.org/W2003840617","https://openalex.org/W2014560186","https://openalex.org/W2017754929","https://openalex.org/W2021035024","https://openalex.org/W2022480925","https://openalex.org/W2028101499","https://openalex.org/W2035575796","https://openalex.org/W2037789705","https://openalex.org/W2053140711","https://openalex.org/W2055214656","https://openalex.org/W2056085087","https://openalex.org/W2061862620","https://openalex.org/W2067635641","https://openalex.org/W2074631079","https://openalex.org/W2075689849","https://openalex.org/W2081066922","https://openalex.org/W2089531178","https://openalex.org/W2115555034","https://openalex.org/W2394740483","https://openalex.org/W2395865990","https://openalex.org/W2409367303","https://openalex.org/W2412876221","https://openalex.org/W2436827832","https://openalex.org/W2463288482","https://openalex.org/W2465829503","https://openalex.org/W2742206604"],"related_works":["https://openalex.org/W1990676347","https://openalex.org/W2061862620","https://openalex.org/W2411135052","https://openalex.org/W2471782202","https://openalex.org/W1978438112","https://openalex.org/W2091588304","https://openalex.org/W2033040659","https://openalex.org/W2085307571","https://openalex.org/W2063899136","https://openalex.org/W2115310323"],"abstract_inverted_index":{"Muscarinic":[0],"acetylcholine":[1],"receptors":[2],"were":[3],"identified":[4],"in":[5,80,90,126,147,222,272],"the":[6,14,18,47,61,72,86,100,107,116,130,161,165,191,203,219,226,230,233,247,256,261,273],"microsomal":[7],"P":[8],"fraction":[9],"of":[10,17,28,39,60,141,160,186,193,197,205,212,232,238,249],"rat":[11],"forebrain":[12],"by":[13,164,190,241,246,276],"specific":[15],"binding":[16,44,105,114],"radiolabeled":[19],"antagonist":[20,104],"[3H]dexetimide.":[21],"Binding":[22],"occurred":[23],"to":[24,106,115,207,235,253,260,268],"a":[25,123,144,157,173,209],"single":[26],"class":[27],"noncooperative":[29],"sites":[30,163,228,240,258,271],"(3.25":[31],"mumol/mg":[32],"protein)":[33],"with":[34,71,255],"an":[35,168,179],"equilibrium":[36],"dissociation":[37],"constant":[38],"1.1":[40],"nM.":[41],"Agonist/[3H]-dexetimide":[42],"competition":[43],"experiments":[45],"allowed":[46],"distinction":[48],"between":[49,218],"two":[50],"major":[51],"muscarinic":[52,251],"receptor":[53,63,102],"subpopulations,":[54],"having":[55],"respectively":[56],"high":[57],"affinity":[58,67,74,81,128,148,175,181,224],"(20%":[59],"total":[62,101],"population)":[64],"and":[65,109,139,229,265],"low":[66],"for":[68,75,84,129,151,176,182,202,225],"agonists,":[69],"but":[70,178,195],"same":[73],"antagonists.":[76,183],"A":[77],"610-fold":[78],"difference":[79],"was":[82,135,153,188],"calculated":[83],"carbamoyl-choline,":[85],"agonist":[87,113,127],"extensively":[88],"investigated":[89],"this":[91],"study.":[92],"The":[93,119,184,215],"alkylating":[94],"reagent":[95,166],"N-ethylmaleimide":[96,242,267],"did":[97],"not":[98,196],"affect":[99],"number,":[103],"high-affinity":[108,117],"low-affinity":[110,131,162,227,257],"sites,":[111],"nor":[112],"sites.":[118,132,214],"reagent,":[120],"however,":[121],"caused":[122],"net":[124],"increase":[125,146,150,221],"This":[133,155],"process":[134],"dependent":[136],"on":[137],"time":[138],"dose":[140],"N-ethylmaleimide,":[142],"until":[143],"maximal":[145],"(fourfold":[149],"carbamoylcholine)":[152],"attained.":[154],"suggests":[156],"quantal":[158],"conversion":[159],"into":[167],"alkylated":[169],"form,":[170],"which":[171,199],"possesses":[172],"higher":[174],"agonists":[177,194,206],"unchanged":[180],"rate":[185],"alkylation":[187,237],"enhanced":[189],"presence":[192],"antagonists,":[198],"is":[200],"indicative":[201],"ability":[204,231,248],"mediate":[208],"conformational":[210],"change":[211],"these":[213,239,270],"close":[216],"correlation":[217],"N-ethylmaleimide-mediated":[220],"drug":[223],"drugs":[234,252],"enhance":[236],"can":[243],"be":[244],"explained":[245],"(a)":[250],"interact":[254],"according":[259],"Monod-Wyman-Changeux":[262],"'Plausible":[263],"Model'":[264],"(b)":[266],"freeze":[269],"'active'":[274],"conformation":[275],"alkylation.":[277]},"counts_by_year":[],"updated_date":"2026-10-31T12:09:11.096373","created_date":"2016-06-24T00:00:00"}
