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PET-evaluated trans...
PET-evaluated transport of [11C]hydroxyurea across the rat blood-brain barrier - : lack of influence of cyc-losporin and probenecid
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- Syvänen, Stina (författare)
- Uppsala Imanet, GE Healthcare,Hammarlund-Udenaes
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Barletta, Julien (författare)
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Blomquist, Gunnar (författare)
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Långström, Bengt (författare)
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Bergström, Mats (författare)
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(creator_code:org_t)
- Bentham Science Publishers Ltd. 2007
- 2007
- Engelska.
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Ingår i: Drug Metabolism Letters. - : Bentham Science Publishers Ltd.. - 1872-3128. ; 1:3, s. 189-194
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.2...
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Abstract
Ämnesord
Stäng
- The transport of hydroxyurea, a ribonucleoside reductase inhibitor, over biological membranes is slow and it has therefore been suggested that the substance could interact with an active efflux transporter. The transport of [11C]hydroxyurea into the rat brain was therefore studied after administration of the multidrug resistance protein inhibitor probenecid (50 and 150 mg/kg), the P-glycoprotein inhibitor cyclosporin A (25 mg/kg), hydroxyurea (50, 150 and 450 mg/kg) and mannitol (25%). None of the intervention drugs affected the brain uptake of [11C]hydroxyurea. The brain-toplasma concentration ratios (Kp), with or without intervention drug, were in the range 0.12-0.25 after 60 min of [11C]hydroxyurea infusion. [11C]Verapamil, a P-glycoprotein substrate with low brain penetration, was used to study the ability of hydroxyurea to inhibit P-glycoprotein. Administration of hydroxyurea (150 and 450 mg/kg) did not increase brain concentrations of [11C]verapamil. It is therefore unlikely that hydroxyurea is a substrate for or an inhibitor of Pglycoprotein or a substrate for a probenecid sensitive transport system. The low brain concentrations may instead be the result of slow uptake due to the hydrophilic nature of hydroxyurea.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Nyckelord
- PET
- [11C]hydroxyurea
- [11C]verapamil
- pharmacokinetics
- blood-brain barrier
- active efflux
- PHARMACY
- FARMACI
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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