ParkinsonFranceV1, PascalFrancis, Checkpoint, bibRecord, 000752

Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood-brain barrier in a rat brain endothelial cell model

Identifieur interne : 000752 ( PascalFrancis/Checkpoint ); précédent : 000751; suivant : 000753

Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood-brain barrier in a rat brain endothelial cell model

Auteurs : Sarah Vautier [France] ; Aline Milane [France] ; Christine Fernandez [France] ; Marion Buyse [France] ; Helene Chacun [France] ; Robert Farinotti [France]

Source :

Neuroscience letters [ 0304-3940 ] ; 2008.

RBID : Pascal:08-0409295

Descripteurs français

Pascal (Inist)
- Antiparkinsonien, Glycoprotéine, Barrière hématoencéphalique, Encéphale, Cellule endothéliale, Modèle, Bromocriptine, Interaction médicamenteuse, Rat, Animal.

English descriptors

KwdEn :
- Animal, Antiparkinson agent, Blood brain barrier, Bromocriptine, Drug interaction, Encephalon, Endothelial cell, Glycoprotein, Models, Rat.

Abstract

Parkinson's disease is a neurodegenerative disorder that requires treatment by dopaminergic agonists, which may be responsible for central side effects. We hypothesized that the efflux transporter ABCB1/P-glycoprotein played a role in brain disposition ofantiparkinsonian drugs and could control central toxicity. We aimed to evaluate antiparkinsonian drugs as ABCB1 substrates and/or inhibitors in rat brain endothelial cells GPNT, in order to predict potential clinical drug-drug interactions. Among the antiparkinsonian drugs tested, levodopa, bromocriptine, pergolide and pramipexole were ABCB1 substrates. However, only bromocriptine could inhibit ABCB1 functionality with an ICso of 6.71 μM on Rhodamine 123 uptake and an IC₅₀ of 1.71 μM on digoxine uptake. Thus, bromocriptine at 100 μM is responsible for an increase of levodopa intracellular transport of about 2.05-fold versus control. Therefore, we can conclude that bromocriptine is a potent drug for medicinal interactions in vitro. Hence, in patients with Parkinson's disease, these results may be considered to optimise treatments individually.

Affiliations:

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Le document en format XML

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<front><div type="abstract" xml:lang="en">Parkinson's disease is a neurodegenerative disorder that requires treatment by dopaminergic agonists, which may be responsible for central side effects. We hypothesized that the efflux transporter ABCB1/P-glycoprotein played a role in brain disposition ofantiparkinsonian drugs and could control central toxicity. We aimed to evaluate antiparkinsonian drugs as ABCB1 substrates and/or inhibitors in rat brain endothelial cells GPNT, in order to predict potential clinical drug-drug interactions. Among the antiparkinsonian drugs tested, levodopa, bromocriptine, pergolide and pramipexole were ABCB1 substrates. However, only bromocriptine could inhibit ABCB1 functionality with an ICso of 6.71 μM on Rhodamine 123 uptake and an IC<sub>50</sub>
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<s5>54</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG"><s0>Rat</s0>
<s5>54</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA"><s0>Rata</s0>
<s5>54</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE"><s0>Animal</s0>
<s5>69</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG"><s0>Animal</s0>
<s5>69</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA"><s0>Animal</s0>
<s5>69</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE"><s0>Système nerveux central</s0>
<s5>20</s5>
</fC07>
<fC07 i1="01" i2="X" l="ENG"><s0>Central nervous system</s0>
<s5>20</s5>
</fC07>
<fC07 i1="01" i2="X" l="SPA"><s0>Sistema nervioso central</s0>
<s5>20</s5>
</fC07>
<fC07 i1="02" i2="X" l="FRE"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="ENG"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="SPA"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="FRE"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="ENG"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="SPA"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="04" i2="X" l="FRE"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="04" i2="X" l="ENG"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="04" i2="X" l="SPA"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fN21><s1>266</s1>
</fN21>
<fN44 i1="01"><s1>OTO</s1>
</fN44>
<fN82><s1>OTO</s1>
</fN82>
</pA>
</standard>
</inist>
<affiliations><list><country><li>France</li>
</country>
<region><li>Île-de-France</li>
</region>
<orgName><li>Université Paris-Sud</li>
</orgName>
</list>
<tree><country name="France"><region name="Île-de-France"><name sortKey="Vautier, Sarah" sort="Vautier, Sarah" uniqKey="Vautier S" first="Sarah" last="Vautier">Sarah Vautier</name>
</region>
<name sortKey="Buyse, Marion" sort="Buyse, Marion" uniqKey="Buyse M" first="Marion" last="Buyse">Marion Buyse</name>
<name sortKey="Chacun, Helene" sort="Chacun, Helene" uniqKey="Chacun H" first="Helene" last="Chacun">Helene Chacun</name>
<name sortKey="Farinotti, Robert" sort="Farinotti, Robert" uniqKey="Farinotti R" first="Robert" last="Farinotti">Robert Farinotti</name>
<name sortKey="Farinotti, Robert" sort="Farinotti, Robert" uniqKey="Farinotti R" first="Robert" last="Farinotti">Robert Farinotti</name>
<name sortKey="Fernandez, Christine" sort="Fernandez, Christine" uniqKey="Fernandez C" first="Christine" last="Fernandez">Christine Fernandez</name>
<name sortKey="Fernandez, Christine" sort="Fernandez, Christine" uniqKey="Fernandez C" first="Christine" last="Fernandez">Christine Fernandez</name>
<name sortKey="Milane, Aline" sort="Milane, Aline" uniqKey="Milane A" first="Aline" last="Milane">Aline Milane</name>
</country>
</tree>
</affiliations>
</record>

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   |texte=   Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood-brain barrier in a rat brain endothelial cell model
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This area was generated with Dilib version V0.6.29.
Data generation: Wed May 17 19:46:39 2017. Site generation: Mon Mar 4 15:48:15 2024

	La maladie de Parkinson en France (serveur d'exploration)
	Attention, ce site est en cours de développement ! Attention, site généré par des moyens informatiques à partir de corpus bruts. Les informations ne sont donc pas validées.

La maladie de Parkinson en France (serveur d'exploration)

Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood-brain barrier in a rat brain endothelial cell model

Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood-brain barrier in a rat brain endothelial cell model

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