Effects of RS 86, an orally active cholinergic agonist, on sleep in man.

The effect of four oral doses of RS 86, a direct-acting cholinergic agonist, on polygraphic sleep parameters was studied in two groups of 12 healthy male volunteers. Subjects received placebo, 0.25 and 0.50 mg (Study I), or placebo, 0.75 and 1.50 mg (Study II), in a double-blind, balanced, crossover design. While 0.25 and 0.50 mg RS 86 had no effect on electrophysiological correlates of sleep, 0.75 and 1.50 mg altered polygraphic sleep parameters in a dose-dependent fashion: the latency of rapid eye movement (REM) sleep was shortened, REM sleep duration in the first third of the sleep period increased, and slow wave sleep reduced in the first and second thirds of the sleep period. Pulse rate was dose-dependently and significantly increased after RS 86. Subjective sleep experience and the subjects' condition in the morning were not altered. These results suggest that RS 86, in well-tolerated oral doses, has central effects that are partly similar to and partly different from those of other cholinomimetic agents.