Penetration of DGAVP (Org 5667) across the blood-brain barrier in human subjects.

To assess the penetration of desglycinamide-arginine-vasopressin (DGAVP, Org 5667) to the central nervous system, levels of DGAVP were measured in the lumbar CSF after peripheral administration. DGAVP (2 mg) was administered intranasally to 37 patients and CSF samples were collected from these patients 5 to 240 minutes later. Detectable levels of DGAVP in CSF could be found 5 minutes after administration, but levels declined rapidly during the next 90 minutes. The DGAVP levels in CSF correlated with plasma levels of DGAVP (r=0.586, p less than 0.001). According to these results, DGAVP may gain access to the central nervous system and may induce central effects.