Interactions between histamine H1 receptor and its antagonists by using cell membrane chromatography method
作者： Jie Zhang , Yanmin Zhang , Weina Ma , Dongdong Zhang , Jing Li
DOI: 10.1111/JPHP.12453
关键词:
摘要: OBJECTIVES A high histamine H1 receptor (H1 R) expression cell membrane chromatography (CMC) method was developed to investigate the affinity of ligands for R. METHODS The R evaluated by frontal analysis. Competition studies and molecular docking study were utilized interactions that occurred at specific binding sites on KEY FINDINGS KD values measured analysis (8.72 ± 0.21) × 10(-7) M azelastine, (9.12 ± 0.26) × 10(-7) cyproheptadine, (9.90 ± 0.18) × 10(-7) doxepin, (1.42 ± 0.13) × 10(-6) astemizole, (2.25 ± 0.36) × 10(-6) chlorpheniramine (3.10 ± 0.27) × 10(-6) diphenhydramine. results had a positive correlation with those from radioligand assay. ability displacement order occupied doxepin (KD , (2.95 ± 0.21) × 10(-8) M) > astemizole (5.03 ± 0.18) × 10(-7) M) > chlorpheniramine (1.27 ± 0.16) × 10(-6) M) > cyproheptadine (1.61 ± 0.27) × 10(-6) M), whose met scores study. CONCLUSIONS showed CMC could be applied drug-receptor interactions.
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