@prefix prodottidellaricerca: . @prefix istituto: . @prefix prodotto: . istituto:CDS061 prodottidellaricerca:prodotto prodotto:ID37618 . @prefix rdf: . prodotto:ID37618 rdf:type prodotto:TIPO1101 . @prefix retescientifica: . prodotto:ID37618 rdf:type retescientifica:ProdottoDellaRicerca . @prefix rdfs: . prodotto:ID37618 rdfs:label "Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. (Articolo in rivista)"@en . @prefix xsd: . @prefix pubblicazioni: . prodotto:ID37618 pubblicazioni:anno "2003-01-01T00:00:00+01:00"^^xsd:gYear . @prefix skos: . prodotto:ID37618 skos:altLabel "
Carbonnelle E, Sparatore F, Canu-Boido C, Salvagno C, Baldani-Guerra B, Terstappen G, Zwart R, Vijverberg H, Clementi F, Gotti C. (2003)
Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes.
in European journal of pharmacology
"^^rdf:HTML ; pubblicazioni:autori "Carbonnelle E, Sparatore F, Canu-Boido C, Salvagno C, Baldani-Guerra B, Terstappen G, Zwart R, Vijverberg H, Clementi F, Gotti C."^^xsd:string ; pubblicazioni:paginaInizio "85"^^xsd:string ; pubblicazioni:paginaFine "96"^^xsd:string ; pubblicazioni:numeroVolume "471"^^xsd:string . @prefix ns9: . prodotto:ID37618 pubblicazioni:rivista ns9:ID393929 ; pubblicazioni:note "IF 2,34 - Citazioni: 1"^^xsd:string ; skos:note "ISI Web of Science (WOS)"^^xsd:string ; pubblicazioni:titolo "Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes."^^xsd:string ; prodottidellaricerca:abstract "Cytisine very potently binds and activates the alpha 3 beta 4 and alpha 7 nicotinic subtypes, but only partially agonises the alpha 4 beta 2 subtype. Although with a lower affinity than cytisine, new cytisine derivatives with different substituents on the basic nitrogen (CC1-CC8) bind to both the heteromeric and homomeric subtypes, with higher affinity for brain [3H]epibatidine receptors. The cytisine derivatives were tested on the Ca(2+) flux of native or transfected cell lines expressing the rat alpha 7, or human alpha 3 beta 4 or alpha 4 beta 2 subtypes using Ca(2+) dynamics in conjunction with a fluorescent image plate reader. None elicited any response at doses of up to 30-100 microM, but all inhibited agonist-induced responses. Compounds CC5 and CC7 were also electrophysiologically tested on oocyte-expressed rat alpha 4 beta 2, alpha 3 beta 4 and alpha 7 subtypes. CC5 competitively antagonised the alpha 4 beta 2 and alpha 3 beta 4 subtypes with similar potency, whereas CC7 only partially agonised them with maximum responses of respectively 3% and 11% of those of 1 mM acetylcholine. Neither compound induced any current in the oocyte-expressed alpha 7 subtype, and both weakly inhibited acetylcholine-induced currents. Adding chemical groups of a different class or size to the basic nitrogen of cytisine leads to compounds that lose full agonist activity on the alpha 3 beta 4 and alpha 7 subtypes." ; prodottidellaricerca:prodottoDi istituto:CDS061 . ns9:ID393929 pubblicazioni:rivistaDi prodotto:ID37618 .