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Rapid analysis of interaction between six drugs and β 2 ‐adrenergic receptor by injection amount‐dependent method
Author(s) -
Zeng Kaizhu,
Wang Jing,
Sun Zhenyu,
Li Qian,
Liao Sha,
Zhao Xinfeng,
Zheng Xiaohui
Publication year - 2017
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.3897
Subject(s) - chemistry , terbutaline , clenbuterol , chromatography , salbutamol , elution , β2 adrenergic receptor , ligand (biochemistry) , receptor , drug , agonist , adrenergic , adrenergic receptor , pharmacology , biochemistry , medicine , asthma
Drug–protein interaction analysis has become a considerable topic in life science which includes clarifying protein functions, explaining drug action mechanisms and uncovering novel drug candidates. This work was to determine the association constants ( K A ) of six drugs to β 2 ‐adrenergic receptor by injection amount‐dependent method using stationary phase containing the immobilized receptor. The values of K A were calculated to be (25.85 ± 0.035) × 10 4 m −1 for clorprenaline, (42.51 ± 0.054) × 10 4 m −1 for clenbuterol, (6.67 ± 0.008) × 10 4 m −1 for terbutaline, (33.99 ± 0.025) × 10 4 m −1 for tulobuterol, (7.59 ± 0.011) × 10 4 m −1 for salbutamol and (78.52 ± 0.087) × 10 4 m −1 for bambuterol. This rank order agreed well with the data determined by zonal elution, frontal analysis and nonlinear chromatography, even using different batches of β 2 ‐AR column. A good correlation was found between the association constants by the current method and radio‐ligand binding assay. Our data indicates that the injection amount‐dependent method is a powerful alternative for rapid analysis of ligand–receptor interactions.