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Binding of 1-[3-(4-tert-butyl-phenoxy)propyl]piperidine, a new non imidazole histamine H3 receptor antagonist to bovine serum albumin
protein binding
equilibrium dialysis
DL76
bovine serum albumin
Bibliogr. s. 1047
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 vitro by equilibrium dialysis at 37OC and pH 7.4 over the concentration range of 0.32ñ317.18 μM and at a physiological protein concentration of 602 μM. 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 μM. Scatchard plot concave-down curve might indicate positive cooperativity, which was confirmed by the Hill plot with the slope higher than one.
dc.abstract.en | 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 vitro by equilibrium dialysis at 37OC and pH 7.4 over the concentration range of 0.32ñ317.18 μM and at a physiological protein concentration of 602 μM. 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 μM. Scatchard plot concave-down curve might indicate positive cooperativity, which was confirmed by the Hill plot with the slope higher than one. | pl |
dc.affiliation | Wydział Farmaceutyczny : Zakład Technologii i Biotechnologii Środków Leczniczych | pl |
dc.affiliation | Wydział Farmaceutyczny : Zakład Biofizyki Farmaceutycznej | pl |
dc.affiliation | Wydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji Fizycznej | pl |
dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Analitycznej | pl |
dc.contributor.author | Szymura-Oleksiak, Joanna - 133617 | pl |
dc.contributor.author | Kryczyk-Poprawa, Agata - 214371 | pl |
dc.contributor.author | Szafarz, Małgorzata - 133549 | pl |
dc.contributor.author | Jawień, Wojciech - 100423 | pl |
dc.contributor.author | Łażewska, Dorota - 159999 | pl |
dc.contributor.author | Kieć-Kononowicz, Katarzyna - 130088 | pl |
dc.date.accession | 2020-07-27 | pl |
dc.date.accessioned | 2020-07-28T05:51:07Z | |
dc.date.available | 2020-07-28T05:51:07Z | |
dc.date.issued | 2012 | pl |
dc.date.openaccess | 0 | |
dc.description.accesstime | w momencie opublikowania | |
dc.description.additional | Bibliogr. s. 1047 | pl |
dc.description.number | 6 | pl |
dc.description.physical | 1043-1047 | pl |
dc.description.publication | 0,42 | pl |
dc.description.version | ostateczna wersja wydawcy | |
dc.description.volume | 69 | pl |
dc.identifier.eissn | 2353-5288 | pl |
dc.identifier.issn | 0001-6837 | pl |
dc.identifier.project | ROD UJ / OP | pl |
dc.identifier.uri | https://ruj.uj.edu.pl/xmlui/handle/item/240426 | |
dc.identifier.weblink | https://www.ptfarm.pl/download/?file=File%2FActa_Poloniae%2F2012%2F6%2F1043.pdf | pl |
dc.language | eng | pl |
dc.language.container | eng | pl |
dc.rights | Udzielam licencji. Uznanie autorstwa - Użycie niekomercyjne 4.0 Międzynarodowa | * |
dc.rights.licence | CC-BY-NC | |
dc.rights.uri | http://creativecommons.org/licenses/by-nc/4.0/legalcode.pl | * |
dc.share.type | otwarte czasopismo | |
dc.subject.en | protein binding | pl |
dc.subject.en | equilibrium dialysis | pl |
dc.subject.en | DL76 | pl |
dc.subject.en | bovine serum albumin | pl |
dc.subtype | Article | pl |
dc.title | Binding of 1-[3-(4-tert-butyl-phenoxy)propyl]piperidine, a new non imidazole histamine H3 receptor antagonist to bovine serum albumin | pl |
dc.title.journal | Acta Poloniae Pharmaceutica. Drug Research | pl |
dc.type | JournalArticle | pl |
dspace.entity.type | Publication |
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