Recent in vitro studies, performed in rat aorta, mesenteric and intrapulmonary arteries, and human pulmonary artery, demonstrated that the β-adrenoceptor ligand CGP-12177A (4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one) is also provided with antagonist or partial agonist properties at α1-adrenoceptors. These observations were supported by estimates of CGP-12177A binding affinity at α1-adrenoceptors, which have been always performed in rat cerebral cortex membranes, as a surrogate of vascular tissue. Since α1D-adrenoceptors are predominant in both rat aorta and mesenteric artery, in the present study, we measured, for the first time, the binding affinity of CGP-12177A at recombinant rat α1D-adrenoceptors expressed in BHK-21 cell membranes. CGP-12177A binding affinity was also determined in rat cerebral cortex membranes, where various α1-adrenoceptor subtypes are present. By means of [3H]prazosin binding competition experiments, we found that CGP-121...
Comparison of the binding affinity of CGP-12177A at recombinant rat α1D-adrenoceptors expressed in BHK-21 cell membranes and α1-adrenoceptors present in rat cerebral cortex membranes
VARANI, Katia;BOREA, Pier Andrea;
2008
Abstract
Recent in vitro studies, performed in rat aorta, mesenteric and intrapulmonary arteries, and human pulmonary artery, demonstrated that the β-adrenoceptor ligand CGP-12177A (4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one) is also provided with antagonist or partial agonist properties at α1-adrenoceptors. These observations were supported by estimates of CGP-12177A binding affinity at α1-adrenoceptors, which have been always performed in rat cerebral cortex membranes, as a surrogate of vascular tissue. Since α1D-adrenoceptors are predominant in both rat aorta and mesenteric artery, in the present study, we measured, for the first time, the binding affinity of CGP-12177A at recombinant rat α1D-adrenoceptors expressed in BHK-21 cell membranes. CGP-12177A binding affinity was also determined in rat cerebral cortex membranes, where various α1-adrenoceptor subtypes are present. By means of [3H]prazosin binding competition experiments, we found that CGP-121...I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
