TY - JOUR
T1 - Characterization of β-adrenoceptors on rat skeletal muscle cells grown in vitro
AU - Disatnik, Marie Helene
AU - Sampson, Sanford R.
AU - Shainberg, Asher
PY - 1990/9/1
Y1 - 1990/9/1
N2 - The binding properties of an hydrophilic β-adrenergic receptor radioligand, (-)[3H](4-(3-tert-butylamino-2-hydroxypropoxy)-benzimidazolo-2-one); ([3H]CGP-12177), were investigated in rat skeletal muscle cells in culture. The binding of [3H]CGP-12177 at 25° was saturable, reversible and of high affinity (Kd = 1.3 ± 0.3 nM). The maximal number of [3H]CGP-12177 binding sites was 30.6 ± 3.2 fmol/dish (34 ± 3.5 fmol/mg protein). β-Adrenergic agonists and antagonists inhibited [3H]CGP-12177 binding. The competing ligand inhibition binding is a typical one for β2-adrenoceptors. The increase in β-adrenoceptors was independent of cell fusion. Amiodarone (10-5 M) decreased the β-adrenoceptor number in skeletal muscle cells differentiated in vitro by 48%, while the affinity for [3H]CGP-12177 was not affected.
AB - The binding properties of an hydrophilic β-adrenergic receptor radioligand, (-)[3H](4-(3-tert-butylamino-2-hydroxypropoxy)-benzimidazolo-2-one); ([3H]CGP-12177), were investigated in rat skeletal muscle cells in culture. The binding of [3H]CGP-12177 at 25° was saturable, reversible and of high affinity (Kd = 1.3 ± 0.3 nM). The maximal number of [3H]CGP-12177 binding sites was 30.6 ± 3.2 fmol/dish (34 ± 3.5 fmol/mg protein). β-Adrenergic agonists and antagonists inhibited [3H]CGP-12177 binding. The competing ligand inhibition binding is a typical one for β2-adrenoceptors. The increase in β-adrenoceptors was independent of cell fusion. Amiodarone (10-5 M) decreased the β-adrenoceptor number in skeletal muscle cells differentiated in vitro by 48%, while the affinity for [3H]CGP-12177 was not affected.
UR - https://www.scopus.com/pages/publications/0025120611
U2 - 10.1016/0006-2952(90)90491-3
DO - 10.1016/0006-2952(90)90491-3
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C2 - 1975171
AN - SCOPUS:0025120611
SN - 0006-2952
VL - 40
SP - 1043
EP - 1048
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 5
ER -