title: Affinity isolation of imidazoline binding proteins from rat brain using 5-amino-efaroxan as a ligand.
abstract: We have employed an amino derivative of the imidazoline ligand, efaroxan, to isolate imidazoline binding proteins from solubilised extracts of rat brain, by affinity chromatography. A number of proteins were specifically retained on the affinity column and one of these was immunoreactive with an antiserum raised against the ion conducting pore component of the ATP-sensitive potassium channel. Patch clamp experiments confirmed that, like its parent compound, amino-efaroxan blocks ATP-sensitive potassium channels in human pancreatic beta-cells and can stimulate the insulin secretion from these cells. The results reveal that a member of the ion conducting pore component family is strongly associated with imidazoline binding proteins in brain and in the endocrine pancreas.
authors.affiliation: Cellular Pharmacology Group, School of Life Sciences, Keele University, Staffordshire, UK.
authors.forename: L K
authors.initials: LK
authors.lastname: Monks
authors.forename: K E
authors.initials: KE
authors.lastname: Cosgrove
authors.forename: M J
authors.initials: MJ
authors.lastname: Dunne
authors.forename: C A
authors.initials: CA
authors.lastname: Ramsden
authors.forename: N G
authors.initials: NG
authors.lastname: Morgan
authors.forename: S L
authors.initials: SL
authors.lastname: Chan
mesh_terms: D018528:ATP-Binding Cassette Transporters; D000818:Animals; D001572:Benzofurans / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D001923:Brain Chemistry; D002846:Chromatography, Affinity / Q000379:methods*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D007515:Islets of Langerhans / Q000166:cytology / Q000378:metabolism; D008024:Ligands; D009419:Nerve Tissue Proteins / Q000302:isolation & purification* / Q000378:metabolism; D018408:Patch-Clamp Techniques; D015221:Potassium Channels / Q000378:metabolism*; D024661:Potassium Channels, Inwardly Rectifying; D011485:Protein Binding; D051381:Rats; D011955:Receptors, Drug / Q000378:metabolism; D064233:Sulfonylurea Receptors
chemical_list: D018528:ATP-Binding Cassette Transporters; D001572:Benzofurans; D007093:Imidazoles; D007328:Insulin; C118759:KU 08C; D008024:Ligands; D009419:Nerve Tissue Proteins; D015221:Potassium Channels; D024661:Potassium Channels, Inwardly Rectifying; D011955:Receptors, Drug; D064233:Sulfonylurea Receptors