PT  - JOURNAL ARTICLE
AU  - Li Di
AU  - John P. Umland
AU  - George Chang
AU  - Youping Huang
AU  - Zhen Lin
AU  - Dennis O. Scott
AU  - Matthew D. Troutman
AU  - Theodore E. Liston
TI  - Species Independence in Brain Tissue Binding Using Brain Homogenates
AID  - 10.1124/dmd.111.038778
DP  - 2011 Jul 01
TA  - Drug Metabolism and Disposition
PG  - 1270--1277
VI  - 39
IP  - 7
4099  - http://dmd.aspetjournals.org/content/39/7/1270.short
4100  - http://dmd.aspetjournals.org/content/39/7/1270.full
SO  - Drug Metab Dispos2011 Jul 01; 39
AB  - Species independence of brain tissue binding was assessed with a large number of structurally diverse compounds using equilibrium dialysis with brain homogenates of seven species and strains (Wistar Han rat, Sprague-Dawley rat, CD-1 mouse, Hartley guinea pig, beagle dog, cynomolgus monkey, and human). The results showed that the fractions unbound of the seven species and strains were strongly correlated with correlation coefficients ranging from 0.93 to 0.99. The cross-species/strain correlations were not significantly different from the interassay correlation with the same species. The linear correlation between Wistar Han and other species had a slope close to 1 and an intercept near 0. Based on orthogonal statistical analysis, no correction is needed for extrapolation of fraction unbound from Wistar Han rat to the other species or strains. Hence, brain tissue binding of Wistar Han rat can be used to obtain binding of other species and strains in drug discovery.