Binding of beta 1-adrenoceptor antagonist [3H]CGP 26505 in rat cerebral cortex and sinus atrial node.
Specific beta 1-adrenoceptors antagonist [3H]CGP 26505 binding was characterized in rat cerebral cortex and heart sinus atrial node. In both tissues [3H]CGP 26505 binding was maximal at 25 degrees C, it was specific, saturable and protein concentration dependent. Scatchard analysis of saturation isotherms of specific [3H]CGP 26505 binding in cerebral cortex showed that [3H]CGP 26505 binds a single class of high affinity sites with a dissociation constant (KD) of 1 +/- 0.3 nM and a maximal number of binding sites (Bmax) of 40 +/- 2 fmol/mg of protein. In sinus atrial node, [3H]-CGP 26505 binds a single class of high affinity sites (KD = 1.9 +/- 0.4 nM, Bmax = 28 +/- 2 fmol/mg of protein).
Chiellini
G
G
Istituto Policattedra di Discipline Biologiche-University of Pisa, Italy.
Giannaccini
G
G
Martini
C
C
Lucacchini
A
A
D000319:Adrenergic beta-Antagonists / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D002540:Cerebral Cortex / Q000378:metabolism*; D007093:Imidazoles / Q000378:metabolism*; D008297:Male; D008565:Membrane Proteins / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D012849:Sinoatrial Node / Q000378:metabolism*; D013696:Temperature
D000319:Adrenergic beta-Antagonists; D007093:Imidazoles; D008565:Membrane Proteins; C049763:CGP 20712A