title: Interactions between histamine H1 receptor and its antagonists by using cell membrane chromatography method.
abstract: OBJECTIVE
  A high histamine H1 receptor (H1 R) expression cell membrane chromatography (CMC) method was developed to investigate the affinity of ligands for H1 R.
  
  
  METHODS
  The affinity of ligands for H1 R was evaluated by frontal analysis. Competition studies and molecular docking study were utilized to study the interactions that occurred at specific binding sites on H1 R.
  
  
  RESULTS
  The KD values measured by frontal analysis were (8.72 ± 0.21) × 10(-7)  M for azelastine, (9.12 ± 0.26) × 10(-7)  M for cyproheptadine, (9.90 ± 0.18) × 10(-7)  M for doxepin, (1.42 ± 0.13) × 10(-6)  M for astemizole, (2.25 ± 0.36) × 10(-6)  M for chlorpheniramine and (3.10 ± 0.27) × 10(-6)  M for diphenhydramine. The results had a positive correlation with those from radioligand binding assay. The ability of displacement order measured on the binding sites occupied by doxepin was doxepin (KD , (2.95 ± 0.21) × 10(-8)  M) > astemizole (KD , (5.03 ± 0.18) × 10(-7)  M) > chlorpheniramine (KD , (1.27 ± 0.16) × 10(-6)  M) > cyproheptadine (KD , (1.61 ± 0.27) × 10(-6)  M), whose order met with the scores by molecular docking study.
  
  
  CONCLUSIONS
  The studies showed CMC could be applied to investigate drug-receptor interactions.
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Weina
authors.initials: W
authors.lastname: Ma
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Dongdong
authors.initials: D
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Delu
authors.initials: D
authors.lastname: Che
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Rui
authors.initials: R
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D002462:Cell Membrane; D002845:Chromatography / Q000379:methods*; D057809:HEK293 Cells; D006634:Histamine H1 Antagonists / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D062105:Molecular Docking Simulation; D011869:Radioligand Assay; D051381:Rats; D011969:Receptors, Histamine H1 / Q000378:metabolism*
chemical_list: D006634:Histamine H1 Antagonists; D008024:Ligands; D011969:Receptors, Histamine H1
keywords: cell membrane chromatography; dissociation equilibrium constant; drug-receptor interactions; frontal analysis; histamine H1 receptor