title: Binding of 1-[3-(4-tert-butyl-phenoxy)propyl]piperidine, a new non imidazole histamine H3 receptor antagonist to bovine serum albumin.
abstract: The degree of binding of a drug to plasma proteins has a significant effect on its distribution, elimination, and pharmacological effect since only the unbound fraction is available for distribution into extra-vascular space. The binding of DL76 (1-[3-(4-tert-butyl-phenoxy)propyl]piperidine) to bovine serum albumin (BSA) was studied in viitro by equilibrium dialysis at 37 degrees C and pH 7.4 over the concentration range of 0.32-317.18 microM and at a physiological protein concentration of 602 microM. Drug concentrations were determined by validated LC/MS/MS method. Nonlinear regression analyses of the data pointed to a single class of binding sites (m = 1) with a dissociation constant of DL76 equal 49.20 microM. Scatchard plot concave-down curve might indicate positive cooperativity, which was confirmed by the Hill plot with the slope higher than one.
authors.affiliation: Department of Pharmacokinetics and Physical Pharmacy, Jagiellonian University Medical College, Kraków, Poland. mfszymur@cyf-kr.edu.pl
authors.forename: Joanna
authors.initials: J
authors.lastname: Szymura-Oleksiak
authors.forename: Agata
authors.initials: A
authors.lastname: Kryczyk
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Szafarz
authors.forename: Wojciech
authors.initials: W
authors.lastname: Jawień
authors.forename: Dorota
authors.initials: D
authors.lastname: Łazewska
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kieć-Kononowicz
mesh_terms: D054828:Histamine H3 Antagonists / Q000378:metabolism*; D010880:Piperidines / Q000378:metabolism*; D011485:Protein Binding; D012710:Serum Albumin, Bovine / Q000378:metabolism*
chemical_list: D054828:Histamine H3 Antagonists; D010880:Piperidines; D012710:Serum Albumin, Bovine