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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

2012
journal article
article
Journal
Acta Poloniae Pharmaceutica. Drug Research
Author
Szymura-Oleksiak Joanna

Kryczyk-Poprawa Agata

Szafarz Małgorzata

Jawień Wojciech

Łażewska Dorota
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Volume
69
Number
6
Pages
1043-1047
ISSN
0001-6837
eISSN
2353-5288
Keywords in English

protein binding

equilibrium dialysis

DL76

bovine serum albumin

URL
https://www.ptfarm.pl/download/?file=File%2FActa_Poloniae%2F2012%2F6%2F1043.pdf
Access date
2020-07-27
Remarks

Bibliogr. s. 1047

Language
English
Journal language
English
Abstract in English

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.

Affiliation
Wydział Farmaceutyczny : Zakład Technologii i Biotechnologii Środków LeczniczychWydział Farmaceutyczny : Zakład Biofizyki FarmaceutycznejWydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji FizycznejWydział Farmaceutyczny : Zakład Chemii Analitycznej
dc.abstract.enThe 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.affiliationWydział Farmaceutyczny : Zakład Technologii i Biotechnologii Środków Leczniczychpl
dc.affiliationWydział Farmaceutyczny : Zakład Biofizyki Farmaceutycznejpl
dc.affiliationWydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji Fizycznejpl
dc.affiliationWydział Farmaceutyczny : Zakład Chemii Analitycznejpl
dc.contributor.authorSzymura-Oleksiak, Joanna - 133617 pl
dc.contributor.authorKryczyk-Poprawa, Agata - 214371 pl
dc.contributor.authorSzafarz, Małgorzata - 133549 pl
dc.contributor.authorJawień, Wojciech - 100423 pl
dc.contributor.authorŁażewska, Dorota - 159999 pl
dc.contributor.authorKieć-Kononowicz, Katarzyna - 130088 pl
dc.date.accession2020-07-27pl
dc.date.accessioned2020-07-28T05:51:07Z
dc.date.available2020-07-28T05:51:07Z
dc.date.issued2012pl
dc.date.openaccess0
dc.description.accesstimew momencie opublikowania
dc.description.additionalBibliogr. s. 1047pl
dc.description.number6pl
dc.description.physical1043-1047pl
dc.description.publication0,42pl
dc.description.versionostateczna wersja wydawcy
dc.description.volume69pl
dc.identifier.eissn2353-5288pl
dc.identifier.issn0001-6837pl
dc.identifier.projectROD UJ / OPpl
dc.identifier.urihttps://ruj.uj.edu.pl/xmlui/handle/item/240426
dc.identifier.weblinkhttps://www.ptfarm.pl/download/?file=File%2FActa_Poloniae%2F2012%2F6%2F1043.pdfpl
dc.languageengpl
dc.language.containerengpl
dc.rightsUdzielam licencji. Uznanie autorstwa - Użycie niekomercyjne 4.0 Międzynarodowa*
dc.rights.licenceCC-BY-NC
dc.rights.urihttp://creativecommons.org/licenses/by-nc/4.0/legalcode.pl*
dc.share.typeotwarte czasopismo
dc.subject.enprotein bindingpl
dc.subject.enequilibrium dialysispl
dc.subject.enDL76pl
dc.subject.enbovine serum albuminpl
dc.subtypeArticlepl
dc.titleBinding of 1-[3-(4-tert-butyl-phenoxy)propyl]piperidine, a new non imidazole histamine H3 receptor antagonist to bovine serum albuminpl
dc.title.journalActa Poloniae Pharmaceutica. Drug Researchpl
dc.typeJournalArticlepl
dspace.entity.typePublication
dc.abstract.enpl
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.affiliationpl
Wydział Farmaceutyczny : Zakład Technologii i Biotechnologii Środków Leczniczych
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Biofizyki Farmaceutycznej
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji Fizycznej
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Analitycznej
dc.contributor.authorpl
Szymura-Oleksiak, Joanna - 133617
dc.contributor.authorpl
Kryczyk-Poprawa, Agata - 214371
dc.contributor.authorpl
Szafarz, Małgorzata - 133549
dc.contributor.authorpl
Jawień, Wojciech - 100423
dc.contributor.authorpl
Łażewska, Dorota - 159999
dc.contributor.authorpl
Kieć-Kononowicz, Katarzyna - 130088
dc.date.accessionpl
2020-07-27
dc.date.accessioned
2020-07-28T05:51:07Z
dc.date.available
2020-07-28T05:51:07Z
dc.date.issuedpl
2012
dc.date.openaccess
0
dc.description.accesstime
w momencie opublikowania
dc.description.additionalpl
Bibliogr. s. 1047
dc.description.numberpl
6
dc.description.physicalpl
1043-1047
dc.description.publicationpl
0,42
dc.description.version
ostateczna wersja wydawcy
dc.description.volumepl
69
dc.identifier.eissnpl
2353-5288
dc.identifier.issnpl
0001-6837
dc.identifier.projectpl
ROD UJ / OP
dc.identifier.uri
https://ruj.uj.edu.pl/xmlui/handle/item/240426
dc.identifier.weblinkpl
https://www.ptfarm.pl/download/?file=File%2FActa_Poloniae%2F2012%2F6%2F1043.pdf
dc.languagepl
eng
dc.language.containerpl
eng
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.enpl
protein binding
dc.subject.enpl
equilibrium dialysis
dc.subject.enpl
DL76
dc.subject.enpl
bovine serum albumin
dc.subtypepl
Article
dc.titlepl
Binding of 1-[3-(4-tert-butyl-phenoxy)propyl]piperidine, a new non imidazole histamine H3 receptor antagonist to bovine serum albumin
dc.title.journalpl
Acta Poloniae Pharmaceutica. Drug Research
dc.typepl
JournalArticle
dspace.entity.type
Publication
Affiliations
No affiliation
Szymura-Oleksiak, Joanna
Kryczyk-Poprawa, Agata
Szafarz, Małgorzata
Jawień, Wojciech
Łażewska, Dorota
Kieć-Kononowicz, Katarzyna

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