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Determination of beta-adrenoceptor subtypes in human pulmonary artery and thoracic aorta by radioligand binding

  
@article{APS8772,
	author = {Hong-Li Peng and Ming-Hua Jiang and Zao-Chen Yang},
	title = {Determination of beta-adrenoceptor subtypes in human pulmonary artery and thoracic aorta by radioligand binding},
	journal = {Acta Pharmacologica Sinica},
	volume = {14},
	number = {4},
	year = {2016},
	keywords = {},
	abstract = {The beta-adrenoceptors of human pulmonary artery (PA) and thoracic aorta (TA) were studied by the use of a high specific activity radioligand [125I]pindolol (Pin). To identify the subtypes of beta-adrenoceptors in the 2 blood vessels, the competitive inhibition curves of [125I]Pin by beta 1-antagonist atenolol and beta 2-agonist salbutamol were analyzed using a computer program LIGAND of a mathematical model of the ligand-binding system. The Bmax (15.3 +/- 1.2 fmol/mg protein) and the dissociation constant Kd (44 +/- 4 pmol.L-1) for PA were similar to those for TA (Bmax, 12.8 +/- 1.2 fmol/mg protein, Kd, 45 +/- 4 pmol.L-1). Competitive inhibition analysis showed that the beta 1- and beta 2-adrenoceptor subtypes coexisted in human PA and TA, with beta 1 adrenoceptor dominant. The ratios of beta 1:beta 2 in PA and TA were 2.9:1.0 and 2.1:1.0, respectively.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/8772}
}