Binding properties of beta-adrenergic receptors in early human fetal lung |
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| Authors: | G Falkay G Németh L Kovács |
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| Affiliation: | 1. Discovery Chemistry and Research Technologies, Eli Lilly and Company, 893 South Delaware Street, Indianapolis, IN 46285, USA;2. Department of Molecular Therapeutics, and Department of Neuroscience, The Scripps Research Institute, Jupiter, FL 33458, USA;1. Toxicology and Biomedicine Research group, Faculty of Applied Sciences, Ton Duc Thang University, Ho Chi Minh City, Vietnam;2. Department of Bioinformatics and Medical Engineering, Asia University, Taichung, Taiwan;3. Cardiovascular research center, Hualien Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, Tzu Chi University of Science and Technology, Hualien, Taiwan;4. Department of Medical Research, China Medical University Hospital, China Medical University, Taichung, Taiwan;5. Department of Biotechnology, Asia University, Taichung, Taiwan |
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| Abstract: | The characteristics of beta-adrenergic receptors in human fetal lung were examined using the beta-adrenoceptor antagonist 3H-dihydroalprenolol /DHA/. Steady-state binding was reached by 15 min at 25 degrees C, and the association and dissociation rate constants were 0.0422 nM-1 min-1 and 0.0874 min-1, respectively. From saturation experiments, Bmax of 82.0 +/- 38 fmol/mg protein and KD = 1.85 +/- 0.92 nM were calculated. Inhibition of 3H-DHA binding by beta-1 /metoprolol/ and beta-2 /zinterol, IPS-339, fenoterol/ selective drugs resulted in biphasic displacement curves with slope factors less than 1.0. Analysis of these curves revealed a beta-1: beta-2 ratio of 40:60 in human fetal lung. The presence of 3H-DHA binding sites in early human lung may have a developmental importance which is not yet understood. |
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