Pituitary localization of 3H-spiroperidol by an uptake/storage mechanism?

The lack of a pituitary imaging agent combined with the considerable clinical value for such an agent prompted an examination of 3H-spiroperidol (3HSp). Spiroperidol was selected for initial evaluation based on its high affinity for D2 receptors which are known to be present in the pituitary. A time course study of 3HSp concentration in rat pituitary and other tissues was conducted. Pituitary activity levels were found to be constant from 5 min to 4 h and were about 8 times levels in corpus striatum at 1 h. Blocking studies with (+) butaclamol and with unlabelled spiroperidol suggested the existence of both a D2 receptor mediated binding localization and a second uptake which is postulated to be an internalization process. Further studies involving ultracentrifugation of pituitary homogenates resulted in evidence for association of 3HSp with dense subcellular particles. 3HSp thus appears to be internalized by pituitary cells.