PMID: 11325192Apr 28, 2001Paper

Profile of ligand binding to the porcine beta2-adrenergic receptor

Journal of Animal Science
W Liang, S E Mills

Abstract

Chinese hamster ovary cells expressing the porcine beta2-adrenergic receptor (betaAR) were used to determine the binding kinetics of agonists and antagonists by competitive displacement of the radioligand [125I]iodocyanopindolol. Several purported agonists, including isoproterenol, epinephrine, norepinephine, dobutamine, salbutamol, and terbutaline, exhibited dual-affinity displacement curves, which is characteristic of agonist binding to betaAR. In each case, the addition of guanosine triphosphate (GTP) eliminated the high-affinity state and resulted in a one-site displacement curve. All of the antagonists modeled to only one site in the presence or absence of GTP. Several ligands, including ones used to promote animal growth (clenbuterol, L-644,969, and ractopamine) and the beta3AR-selective agonist BRL 37344 modeled to only one site, suggesting that these ligands would not be full agonists at the porcine beta2AR (pbeta2AR). Most of the tested ligands exhibited binding affinities that were similar to published values for the beta2AR from other species. However, several exceptions were observed. The BRL 37344 ligand bound the pbeta2AR with a 10-fold higher affinity than the human beta2AR, and the Kd of this was similar to Kd v...Continue Reading

Citations

Feb 25, 2003·Journal of Animal Science·S E MillsD J Smith
Oct 8, 2005·Biology of the Neonate·Rashmi ChandraDona M Chikaraishi
Mar 29, 2003·Journal of Animal Science·S E MillsD J Smith
Jan 5, 2011·Journal of Molecular Modeling·Marvin A Soriano-UrsúaAlberto J Kaumann
Mar 10, 2009·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Xinfeng ZhaoWeijin Zang

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