In vitro binding of chloroquine to rat muscle preparations.

Abstract:

:Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentrations of free CQ greatly exceeding toxic plasma levels. Cell structural integrity is not essential for uptake, indicating that CQ is bound to tissue constituents and not trapped inside cells by an active process. At pH 7.4, binding of ionized CQ at anionic sites on tissue predominates over lipid partitioning of the un-ionized species. Binding to phospholipids is a major component of total muscle binding.

journal_name

J Pharm Sci

authors

MacIntyre AC,Cutler DJ

doi

10.1002/jps.2600751109

subject

Has Abstract

pub_date

1986-11-01 00:00:00

pages

1068-70

issue

11

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)47264-8

journal_volume

75

pub_type

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