Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity.

A series of 7-oxaaporphine derivatives was prepared. The compounds were evaluated as dopaminergic agents. None of them showed either affinity for dopamine receptors or activity in vivo in the climbing behavior (mice) and turning behavior (6-hydroxydopamine-lesioned rats) tests.

Receptor adaptive responsiveness in disease models: 6-OHDA lesioned and spontaneously hypertensive rats.

We have examined the adaptive modifications of brain monoamine receptors in response to pathophysiological processes in animal disease models: 6-OHDA lesioned and spontaneously hypertensive rats (SHR). The two models share a similar increase in D-1 receptor densities, while noradrenergic receptors are affected in different way: alpha-1 and beta are supersensitive in 6-OHDA lesioned rats and only alpha-2 are increased in SHR. S-1 receptors too are up-regulated in SHR.

[A review of pharmacological studies on nicergoline].

10-Methoxy-1,6-dimethyl-ergoline-8 beta-methanol-(5-bromonicotinate) (nicergoline, Sermion) shows a strong alpha-blocking activity both in vitro and in vivo. Various studies (dog, cat, rabbit, rat, mouse, guinea-pig) show that nicergoline affects only slightly blood pressure and heart rate and increases the blood flow in brain and hind limb without affecting the splanchnic and aortic flow in normal animals. Nicergoline does not interfere with CNS functions unless applied in high doses.