Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier
Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as p...
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| Autor*in: |
Bourasset, Fanchon [verfasserIn] Cisternino, Salvatore [verfasserIn] Temsamani, Jamal [verfasserIn] |
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| Format: |
E-Artikel |
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| Erschienen: |
Oxford, UK: Blackwell Science Ltd ; 2003 |
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| Schlagwörter: |
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| Umfang: |
Online-Ressource |
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| Reproduktion: |
2003 ; Blackwell Publishing Journal Backfiles 1879-2005 |
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| Übergeordnetes Werk: |
In: Journal of neurochemistry - Oxford : Wiley-Blackwell, 1956, 86(2003), 6, Seite 0 |
| Übergeordnetes Werk: |
volume:86 ; year:2003 ; number:6 ; pages:0 |
| Links: |
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| DOI / URN: |
10.1046/j.1471-4159.2003.01990.x |
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NLEJ243127618 |
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| 520 | |a Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. | ||
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10.1046/j.1471-4159.2003.01990.x doi (DE-627)NLEJ243127618 DE-627 ger DE-627 rakwb Bourasset, Fanchon verfasserin aut Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier Oxford, UK Blackwell Science Ltd 2003 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. 2003 Blackwell Publishing Journal Backfiles 1879-2005 |2003|||||||||| blood–brain barrier Cisternino, Salvatore verfasserin aut Temsamani, Jamal verfasserin aut Scherrmann, Jean-Michel oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 86(2003), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:86 year:2003 number:6 pages:0 http://dx.doi.org/10.1046/j.1471-4159.2003.01990.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 86 2003 6 0 |
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10.1046/j.1471-4159.2003.01990.x doi (DE-627)NLEJ243127618 DE-627 ger DE-627 rakwb Bourasset, Fanchon verfasserin aut Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier Oxford, UK Blackwell Science Ltd 2003 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. 2003 Blackwell Publishing Journal Backfiles 1879-2005 |2003|||||||||| blood–brain barrier Cisternino, Salvatore verfasserin aut Temsamani, Jamal verfasserin aut Scherrmann, Jean-Michel oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 86(2003), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:86 year:2003 number:6 pages:0 http://dx.doi.org/10.1046/j.1471-4159.2003.01990.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 86 2003 6 0 |
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10.1046/j.1471-4159.2003.01990.x doi (DE-627)NLEJ243127618 DE-627 ger DE-627 rakwb Bourasset, Fanchon verfasserin aut Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier Oxford, UK Blackwell Science Ltd 2003 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. 2003 Blackwell Publishing Journal Backfiles 1879-2005 |2003|||||||||| blood–brain barrier Cisternino, Salvatore verfasserin aut Temsamani, Jamal verfasserin aut Scherrmann, Jean-Michel oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 86(2003), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:86 year:2003 number:6 pages:0 http://dx.doi.org/10.1046/j.1471-4159.2003.01990.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 86 2003 6 0 |
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10.1046/j.1471-4159.2003.01990.x doi (DE-627)NLEJ243127618 DE-627 ger DE-627 rakwb Bourasset, Fanchon verfasserin aut Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier Oxford, UK Blackwell Science Ltd 2003 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. 2003 Blackwell Publishing Journal Backfiles 1879-2005 |2003|||||||||| blood–brain barrier Cisternino, Salvatore verfasserin aut Temsamani, Jamal verfasserin aut Scherrmann, Jean-Michel oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 86(2003), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:86 year:2003 number:6 pages:0 http://dx.doi.org/10.1046/j.1471-4159.2003.01990.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 86 2003 6 0 |
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10.1046/j.1471-4159.2003.01990.x doi (DE-627)NLEJ243127618 DE-627 ger DE-627 rakwb Bourasset, Fanchon verfasserin aut Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier Oxford, UK Blackwell Science Ltd 2003 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. 2003 Blackwell Publishing Journal Backfiles 1879-2005 |2003|||||||||| blood–brain barrier Cisternino, Salvatore verfasserin aut Temsamani, Jamal verfasserin aut Scherrmann, Jean-Michel oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 86(2003), 6, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:86 year:2003 number:6 pages:0 http://dx.doi.org/10.1046/j.1471-4159.2003.01990.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 86 2003 6 0 |
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Bourasset, Fanchon Cisternino, Salvatore Temsamani, Jamal |
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Elektronische Aufsätze |
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Bourasset, Fanchon |
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10.1046/j.1471-4159.2003.01990.x |
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verfasserin |
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evidence for an active transport of morphine-6-β-d-glucuronide but not p-glycoprotein-mediated at the blood–brain barrier |
| title_auth |
Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier |
| abstract |
Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. |
| abstractGer |
Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. |
| abstract_unstemmed |
Morphine-6-β-d-glucuronide (M6G) is an active metabolite of morphine with high analgesic potency despite a low blood–brain barrier (BBB) permeability. The aim of the study was to elucidate its transport mechanism across the BBB. We first checked if M6G was effluxed by the P-glycoprotein (P-gp), as previously reported by others. Second, we investigated the role of anionic transporters like the multidrug resistance-associated protein mrp1 and the glucose transporter GLUT-1. The brain uptake of [14C]M6G was measured by the in situ brain perfusion technique in wild-type and deficient mice [mdr1a(–/–) and mrp1(–/–)], with and without probenecid, digoxin, PSC833 or d-glucose. No difference was found between P-gp and mrp1 competent and deficient mice. The brain uptake of [14C]M6G co-perfused with probenecid in wild-type mice was not significantly different from that found in group perfused with [14C]M6G alone. The co-perfusion of [14C]M6G with digoxin or PSC833 was responsible of a threefold decrease of its uptake in mdr1a competent and deficient mice, suggesting that another transporter than P-gp and sensitive to digoxin and PSC833, may be involved. The co-perfusion of [14C]M6G with d-glucose revealed a threefold decrease in M6G uptake. In conclusion, P-gp and mrp1 are not involved in the transport of M6G at the BBB level in contrast to GLUT-1 and a digoxin-sensitive transporter (probably oatp2), which can actively transport M6G but with a weak capacity. |
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| title_short |
Evidence for an active transport of morphine-6-β-d-glucuronide but not P-glycoprotein-mediated at the blood–brain barrier |
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Cisternino, Salvatore Temsamani, Jamal Scherrmann, Jean-Michel |
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