A method of computing drug distribution in plasma using stepwise association constants: Clofibrate acid as an illustrative example

Oleate uptake by cardiac myocytes is carrier mediated and involves a 40-kD plasma membrane fatty acid binding protein similar to that in liver, adipose tissue, and gut.

“…Over a wide range of absolute concentrations of oleate and BSA, the concentration of unbound oleate is precisely determined by the oleate/albumin molar ratio (18,19). Nevertheless, at low and nonphysiologic oleate/albumin concentrations the velocity of hepatocellular oleate uptake increases with increasing concentrations of substrate, despite a fixed molar ratio (22, 23).…”

Uptake of long-chain fatty acids in HepG2 cells involves caveolae

“…Radioactivity was determined after the addition of 10 ml Ultima-Gold (Packard, Groningen, The Netherlands) in a 1,217 Rackbeta liquid scintillation counter (LKBWallac, Turku, Finland). The concentrations of unbound fatty acids in [ 3 H]oleic acid/albumin solutions (fixed BSA concentration ϭ 173 mol/l, oleic acid:BSA molar ratios ranging from 0.1 to 2) were calculated by the stepwise equilibrium constant of Wosilait and Nagy (27), using the dissociation constants for the oleic acid/albumin complex reported by Spector et al (28).…”

Evidence for vesicles that mediate long-chain fatty acid uptake by human microvascular endothelial cells

“…The concentrations of unbound fatty acids in [ 3 H]oleate-BSA solutions (fixed BSA concentration ϭ 173 mol/l, oleate:BSA molar ratios ranging from 0.1 to 2) were calculated by the stepwise equilibrium constant of Wosilait and Nagy (12), using the dissociation constants for the oleate-albumin complex reported by Spector et al (13).…”