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Statements

Subject Item
n2:RIV%2F62157124%3A16370%2F13%3A43872326%21RIV14-MSM-16370___
rdf:type
skos:Concept n17:Vysledek
dcterms:description
The log BB parameter is the logarithm of the ratio of a compound's equilibrium concentrations in the brain tissue versus the blood plasma. This parameter is a useful descriptor in assessing the ability of a compound to permeate the blood-brain barrier. The aim of this study was to develop a Hansch-type linear regression QSAR model that correlates the parameter log BB and the retention time of drugs and other organic compounds on a reversed-phase HPLC containing an embedded amide moiety. The retention time was expressed by the capacity factor log k'. The second aim was to estimate the brain's absorption of 2-(azacycloalkyl)acetamidophenoxyacetic acids, which are analogues of piracetam, nefiracetam, and meclofenoxate. Notably, these acids may be novel nootropics. Two simple regression models that relate log BB and log k' were developed from an assay performed using a reversed-phase HPLC that contained an embedded amide moiety. Both the quadratic and linear models yielded statistical parameters comparable to previously published models of log BB dependence on various structural characteristics. The models predict that four members of the substituted phenoxyacetic acid series have a strong chance of permeating the barrier and being absorbed in the brain. The results of this study show that a reversed-phase HPLC system containing an embedded amide moiety is a functional in vitro surrogate of the blood-brain barrier. These results suggest that racetam-type nootropic drugs containing a carboxylic moiety could be more poorly absorbed than analogues devoid of the carboxyl group, especially if the compounds penetrate the barrier by a simple diffusion mechanism. The log BB parameter is the logarithm of the ratio of a compound's equilibrium concentrations in the brain tissue versus the blood plasma. This parameter is a useful descriptor in assessing the ability of a compound to permeate the blood-brain barrier. The aim of this study was to develop a Hansch-type linear regression QSAR model that correlates the parameter log BB and the retention time of drugs and other organic compounds on a reversed-phase HPLC containing an embedded amide moiety. The retention time was expressed by the capacity factor log k'. The second aim was to estimate the brain's absorption of 2-(azacycloalkyl)acetamidophenoxyacetic acids, which are analogues of piracetam, nefiracetam, and meclofenoxate. Notably, these acids may be novel nootropics. Two simple regression models that relate log BB and log k' were developed from an assay performed using a reversed-phase HPLC that contained an embedded amide moiety. Both the quadratic and linear models yielded statistical parameters comparable to previously published models of log BB dependence on various structural characteristics. The models predict that four members of the substituted phenoxyacetic acid series have a strong chance of permeating the barrier and being absorbed in the brain. The results of this study show that a reversed-phase HPLC system containing an embedded amide moiety is a functional in vitro surrogate of the blood-brain barrier. These results suggest that racetam-type nootropic drugs containing a carboxylic moiety could be more poorly absorbed than analogues devoid of the carboxyl group, especially if the compounds penetrate the barrier by a simple diffusion mechanism.
dcterms:title
Chromatographic behaviour predicts the ability of potential nootropics to permeate the blood-brain barrier. Chromatographic behaviour predicts the ability of potential nootropics to permeate the blood-brain barrier.
skos:prefLabel
Chromatographic behaviour predicts the ability of potential nootropics to permeate the blood-brain barrier. Chromatographic behaviour predicts the ability of potential nootropics to permeate the blood-brain barrier.
skos:notation
RIV/62157124:16370/13:43872326!RIV14-MSM-16370___
n17:predkladatel
n18:orjk%3A16370
n3:aktivita
n6:V
n3:aktivity
V
n3:cisloPeriodika
1
n3:dodaniDat
n11:2014
n3:domaciTvurceVysledku
n5:6364691
n3:druhVysledku
n15:J
n3:duvernostUdaju
n10:S
n3:entitaPredkladatele
n14:predkladatel
n3:idSjednocenehoVysledku
65394
n3:idVysledku
RIV/62157124:16370/13:43872326
n3:jazykVysledku
n16:eng
n3:klicovaSlova
RP-HPLC; Nootropics; Hansch analysis; Embedded amide moiety; Blood-brain barrier
n3:klicoveSlovo
n4:Embedded%20amide%20moiety n4:RP-HPLC n4:Hansch%20analysis n4:Nootropics n4:Blood-brain%20barrier
n3:kodStatuVydavatele
AT - Rakouská republika
n3:kontrolniKodProRIV
[0709F8D79578]
n3:nazevZdroje
Scientia Pharmaceutica
n3:obor
n19:FR
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
1
n3:rokUplatneniVysledku
n11:2013
n3:svazekPeriodika
81
n3:tvurceVysledku
Farsa, Oldřich
s:issn
0036-8709
s:numberOfPages
11
n9:doi
10.3797/scipharm.1208-19
n12:organizacniJednotka
16370