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dc.contributor.author
Talevi, Alan
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dc.contributor.author
Bellera, Carolina Leticia
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dc.contributor.other
Talevi, Alan
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dc.date.available
2023-01-30T13:38:48Z
dc.date.issued
2021
dc.identifier.citation
Talevi, Alan; Bellera, Carolina Leticia; Unbound brain-to-plasma partition coefficient determination; Springer Nature Switzerland AG; 2021; 1-8
dc.identifier.isbn
978-3-030-51519-5
dc.identifier.uri
http://hdl.handle.net/11336/186081
dc.description.abstract
The unbound brain-to-plasma concentration ratio (or unboundbrain-to-plasma ratio, Kp,uu) reflects the partition of unbound drug betweenthe brain and the plasma, at steady state.where Cu,brain,ss is the unbounddrug concentration in the brain, at steady state, and Cu,blood,ss is the unbunddrug concentration in blood, at steady state. It is a critical parameterto evaluate if the distribution (pseudo)equilibrium between blood and braincompartments has been achieved, reflecting the joint impact of passivepermeability and transporters at the blood-brain barrier. Furthermore, it doesnot depend on protein binding in blood or binding to brain tissue constituents.(the bound fraction in blood and the brain is pharmacologically inert; theunbound or free fraction, in contrast, is able to diffuse trough physiologicalbarriers and engage with the target). As the unbound fraction is more relevantfrom a pharmacological viewpoint, Kp,uu is at present considered one of themost relevant parameters to guide the selection and optimization of centralnervous system (CNS) drug candidates (usually preferring compounds withcomparatively high Kp,uu values). Contrariwise, it may also be used during thescreening of peripheral drugs, since minimizing unbound exposure in the brainmight reduce the incidence of central side effects. Microdialysis is currentlythe gold standard for Kp,uu determinations, although other less complextechniques with better throughput have also been proposed. Also, in silicomethods for Kp,uu estimation have increasingly appeared in the specializedliterature.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Springer Nature Switzerland AG
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
UNBOUND BRAIN-TO-PLASMA CONCENTRATION RATIO
dc.subject
UNBOUND BRAIN-TO-PLASMA RATIO
dc.subject.classification
Otras Ciencias Biológicas
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dc.subject.classification
Ciencias Biológicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Unbound brain-to-plasma partition coefficient determination
dc.type
info:eu-repo/semantics/publishedVersion
dc.type
info:eu-repo/semantics/bookPart
dc.type
info:ar-repo/semantics/parte de libro
dc.date.updated
2022-12-06T11:21:29Z
dc.journal.pagination
1-8
dc.journal.pais
Reino Unido
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dc.journal.ciudad
Basignstoke
dc.description.fil
Fil: Talevi, Alan. Universidad Nacional de La Plata. Facultad de Ciencas Exactas. Laboratorio de Investigación y Desarrollo de Bioactivos; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina
dc.description.fil
Fil: Bellera, Carolina Leticia. Universidad Nacional de La Plata. Facultad de Ciencas Exactas. Laboratorio de Investigación y Desarrollo de Bioactivos; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://doi.org/10.1007/978-3-030-51519-5_62-1
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://link.springer.com/referenceworkentry/10.1007/978-3-030-51519-5_62-1
dc.conicet.paginas
1500
dc.source.titulo
The ADME encyclopedia: A comprehensive guide on biopharmacy and pharmacokinetics
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