title: Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
abstract: The binding affinities of agonists at heteromeric nicotinic receptors composed of rat alpha2, alpha3 and alpha4 subunits in combination with beta2 or beta4 subunits were examined in stably transfected HEK 293 cells. In most cases, the affinities of agonists were higher at receptors composed of an alpha subunit in combination with the beta2 subunit than the beta4 subunit, and in some cases this difference was quite large (>250 times), suggesting the possibility of developing subtype-selective ligands and therapeutically useful drugs.
authors.affiliation: Department of Pharmacology, Georgetown University School of Medicine, Washington, DC 20057, USA.
authors.forename: Yingxian
authors.initials: Y
authors.lastname: Xiao
authors.forename: Maryna
authors.initials: M
authors.lastname: Baydyuk
authors.forename: Haizhu Pearl
authors.initials: HP
authors.lastname: Wang
authors.forename: Heather E
authors.initials: HE
authors.lastname: Davis
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Kellar
mesh_terms: D000818:Animals; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D015870:Gene Expression / Q000187:drug effects; D006801:Humans; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D018722:Nicotinic Agonists / Q000494:pharmacology*; D021122:Protein Subunits / Q000187:drug effects / Q000235:genetics / Q000378:metabolism; D051381:Rats; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D014162:Transfection
chemical_list: D018722:Nicotinic Agonists; D021122:Protein Subunits; D011978:Receptors, Nicotinic