title: [125I]BE 2254, a new high affinity radioligand for alpha 1-adrenoceptors.
abstract: [125I]BE 2254 (IBE 2254), a new iodinated radioligand of high specific radioactivity (2175 Ci/mmol) was developed and used to characterize alpha 1-adrenoceptors in rat cerebral cortex membranes. IBE 2254 possessed a high affinity, KD 78 +/- 14 pM with a Bmax of 210 +/- 26 fmol/mg and 90% specific binding at KD value. alpha-Adrenergic antagonists competed for IBE 2254 binding in the following order: prazosin greater than or equal to WB 4101 greater than phentolamine greater than corynanthine greater than yohimbine greater than rauwolscine, a strong indication that IBE 2254 binds to alpha 1-adrenoceptors. IBE 2254 appears to be a very useful tool for studying alpha 1-adrenoceptors.
mesh_terms: D000818:Animals; D007457:Iodine Radioisotopes; D008297:Male; D010627:Phenethylamines; D011869:Radioligand Assay; D051381:Rats; D011941:Receptors, Adrenergic / Q000032:analysis*; D011942:Receptors, Adrenergic, alpha / Q000032:analysis*; D044024:Tetralones
chemical_list: D007457:Iodine Radioisotopes; D010627:Phenethylamines; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D044024:Tetralones; C010652:BE 2254