Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats

Abstract The unbound concentrations of 14 commercial drugs, including five non‐efflux/uptake transporter substrates—Class I, five efflux transporter substrates—class II and four influx transporter substrates—Class III, were simultaneously measured in rat liver, muscle, and blood via microanalysis. K...

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Autores principales:	Shuyao Wang, Chun Chen, Chi Guan, Liping Qiu, Lei Zhang, Shaofeng Zhang, Hongyu Zhou, Hongwen Du, Chen Li, Yaqiong Wu, Hang Chang, Tao Wang
Formato:	article
Lenguaje:	EN
Publicado:	Wiley 2021
Materias:	asymmetrically distributed cell metabolism membrane transport microanalysis unbound drug concentration Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/888cbe7245f6422fa500b10c7fc1165f
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spelling	oai:doaj.org-article:888cbe7245f6422fa500b10c7fc1165f2021-11-16T13:45:56ZEffects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats2052-170710.1002/prp2.879https://doaj.org/article/888cbe7245f6422fa500b10c7fc1165f2021-10-01T00:00:00Zhttps://doi.org/10.1002/prp2.879https://doaj.org/toc/2052-1707Abstract The unbound concentrations of 14 commercial drugs, including five non‐efflux/uptake transporter substrates—Class I, five efflux transporter substrates—class II and four influx transporter substrates—Class III, were simultaneously measured in rat liver, muscle, and blood via microanalysis. Kpuu,liver and Kpuu,muscle were calculated to evaluate the membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver. For Class I compounds, represented by antipyrine, unbound concentrations among liver, muscle and blood are symmetrically distributed when compound hepatic clearance is low. And when compound hepatic clearance is high, unbound concentrations among liver, muscle and blood are asymmetrically distributed, such as Propranolol. For Class II and III compounds, overall, the unbound concentrations among liver, muscle, and blood are asymmetrically distributed due to a combination of hepatic metabolism and efflux and/or influx transporter activity.Shuyao WangChun ChenChi GuanLiping QiuLei ZhangShaofeng ZhangHongyu ZhouHongwen DuChen LiYaqiong WuHang ChangTao WangWileyarticleasymmetrically distributedcell metabolismmembrane transportmicroanalysisunbound drug concentrationTherapeutics. PharmacologyRM1-950ENPharmacology Research & Perspectives, Vol 9, Iss 5, Pp n/a-n/a (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	asymmetrically distributed cell metabolism membrane transport microanalysis unbound drug concentration Therapeutics. Pharmacology RM1-950
spellingShingle	asymmetrically distributed cell metabolism membrane transport microanalysis unbound drug concentration Therapeutics. Pharmacology RM1-950 Shuyao Wang Chun Chen Chi Guan Liping Qiu Lei Zhang Shaofeng Zhang Hongyu Zhou Hongwen Du Chen Li Yaqiong Wu Hang Chang Tao Wang Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats
description	Abstract The unbound concentrations of 14 commercial drugs, including five non‐efflux/uptake transporter substrates—Class I, five efflux transporter substrates—class II and four influx transporter substrates—Class III, were simultaneously measured in rat liver, muscle, and blood via microanalysis. Kpuu,liver and Kpuu,muscle were calculated to evaluate the membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver. For Class I compounds, represented by antipyrine, unbound concentrations among liver, muscle and blood are symmetrically distributed when compound hepatic clearance is low. And when compound hepatic clearance is high, unbound concentrations among liver, muscle and blood are asymmetrically distributed, such as Propranolol. For Class II and III compounds, overall, the unbound concentrations among liver, muscle, and blood are asymmetrically distributed due to a combination of hepatic metabolism and efflux and/or influx transporter activity.
format	article
author	Shuyao Wang Chun Chen Chi Guan Liping Qiu Lei Zhang Shaofeng Zhang Hongyu Zhou Hongwen Du Chen Li Yaqiong Wu Hang Chang Tao Wang
author_facet	Shuyao Wang Chun Chen Chi Guan Liping Qiu Lei Zhang Shaofeng Zhang Hongyu Zhou Hongwen Du Chen Li Yaqiong Wu Hang Chang Tao Wang
author_sort	Shuyao Wang
title	Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats
title_short	Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats
title_full	Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats
title_fullStr	Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats
title_full_unstemmed	Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats
title_sort	effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: a microdialysis study in rats
publisher	Wiley
publishDate	2021
url	https://doaj.org/article/888cbe7245f6422fa500b10c7fc1165f
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Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats

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