Allosteric modulation of peripheral sigma binding sites by a new selective ligand: SR 31747.

The interactions of a new compound SR 31747 with sigma sites were examined in rat spleen membranes and in human peripheral blood leukocytes (PBL). Nanomolar concentrations of SR 31747 selectively inhibited in a non-competitive manner the binding of the prototypic sigma ligands [3H](+)-pentazocine, [3H](+)-3PPP and [3H]DTG on rat spleen membranes. Characterization of SR 31747 binding sites using [3H]SR 31747 as a ligand showed that this compound binds reversibly, with high affinity to one class of sites on rat spleen membranes (Kd 0.

Effect of pentosan polysulphate on endothelial regeneration.

Endothelium was removed from rabbit aortae using a balloon catheter and the endothelial outgrowth was measured. In the controls, after initial regrowth of approximately 4 weeks, endothelial regeneration stopped before cellular regrowth was complete. However, when treated with daily subcutaneous injections of pentosan polysulphate (PPS) (8 mg/kg/day), endothelium fully repopulated the denuded areas 16 weeks after beginning of the treatment.