Original Article

Changes in adrenal benzodiazepine receptors in spontaneously hypertensive rats

Authors: Lie-chang SONG, Ting-chong ZHOU


[3H]PK-11195[1-(2-chlorophenyl)-N-methyl-N-(1-methyl [2,3-3H]propyl)-3-isoquinolinecarboxamide] is a labeled ligand with high affinity selectively binding to “peripheral type” benzodiazepine receptors. The kinetic constants of [3H]PK-11195 binding to the adrenal homogenates of spontaneously hypertensive rats (WKY) were measured. Scatchard analysis of the specific binding showed a single class of binding site with a maximal capacity (Bmax) of 11.9+/-1.7 and 22.8+/-1.9 pmol/mg protein for SHR and WKY, and an apparent equilibrium dissociation constant (KD) of 8.1+/-1.9 and 8.6+/-1.9 nM for SHR and WKY, respectively.
These results demonstrated that the adrenal benzodiazepine binding sites in SHR are less than those in WKY, but the affinities are similar.

Article Options

Download Citation

Cited times in Scopus