Understanding the pharmacokinetics of synthetic cathinones: Evaluation of the blood–brain barrier permeability of 13 related compounds in rats
Impact
Scholar |
Other documents of the author: Fabregat-Safont, David; Barneo-Muñoz, Manuela; Carbón, Xoán; Hernandez, Felix; Martinez-Garcia, Fernando; Ventura, Mireia; Stove, Christophe P.; Sancho, Juan V; Ibáñez, Maria
Metadata
Show full item recordcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/33596
comunitat-uji-handle3:10234/33597
comunitat-uji-handle4:
INVESTIGACIONMetadata
Title
Understanding the pharmacokinetics of synthetic cathinones: Evaluation of the blood–brain barrier permeability of 13 related compounds in ratsAuthor (s)
Date
2020Publisher
WileyISSN
1355-6215; 1369-1600Bibliographic citation
Fabregat‐Safont, D, Barneo‐Muñoz, M, Carbón, X, et al. Understanding the pharmacokinetics of synthetic cathinones: Evaluation of the blood–brain barrier permeability of 13 related compounds in rats. Addiction Biology. 2020;e12979. https://doi.org/10.1111/adb.12979Type
info:eu-repo/semantics/articlePublisher version
https://onlinelibrary.wiley.com/doi/10.1111/adb.12979Version
info:eu-repo/semantics/submittedVersionSubject
Abstract
Synthetic cathinones are the second most commonly seized new psychoactive substance family in Europe. These compounds have been related to several intoxication cases, including fatalities. Although the pharmacological ... [+]
Synthetic cathinones are the second most commonly seized new psychoactive substance family in Europe. These compounds have been related to several intoxication cases, including fatalities. Although the pharmacological effects, metabolism, and pharmacokinetics of cathinones have been studied, there is little information about the permeability of these compounds through the blood–brain barrier (BBB). This is an important parameter to understand the behavior and potency of cathinones. In this work, 13 selected cathinones have been analyzed in telencephalon tissue from Sprague–Dawley rats intraperitoneally dosed at 3 mg/kg. Our results revealed a direct relationship between compound polarity and BBB permeability, with higher permeability for the more polar cathinones. The chemical moieties present in the cathinone had an important impact on the BBB permeability, with lengthening of the α‐alkyl chain or functionalization of the aromatic ring with alkyl moieties resulting in lower concentration in telencephalon tissue. Our data suggest that transport of cathinones is a carrier‐mediated process, similar to cocaine transport across the BBB. [-]
Description
This is the pre-peer reviewed version of the following article:Understanding the pharmacokinetics of synthetic cathinones: Evaluation of the blood–brain barrier permeability of 13 related compounds in rats, which has ... [+]
This is the pre-peer reviewed version of the following article:Understanding the pharmacokinetics of synthetic cathinones: Evaluation of the blood–brain barrier permeability of 13 related compounds in rats, which has been published in final form at https://doi.org/10.1111/adb.12979. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions. [-]
Is part of
Addiction Biology, 2020Funder Name
Universitat Jaume I de Castelló, Grant/Award Number: UJI‐B2016‐45; Generalitat Valenciana, Grant/Award Number: PROMETEO/2016/076; Ministerio de Economía y Competitividad‐FEDER, Grant/Award Number: (BFU2016‐77691‐C2‐1‐P; Ministerio de Educación, Cultura y Deporte, Grant/Award Number: FPU15/02033; University Jaume I, Grant/Award Number: UJI‐B2018‐19
Rights
Copyright © John Wiley & Sons, Inc.
http://rightsstatements.org/vocab/InC/1.0/
info:eu-repo/semantics/openAccess
http://rightsstatements.org/vocab/InC/1.0/
info:eu-repo/semantics/openAccess
This item appears in the folowing collection(s)
- IUPA_Articles [309]