title: Vesamicol, an acetylcholine uptake blocker in presynaptic vesicles, suppresses rapid eye movement (REM) sleep in the rat.
abstract: Vesamicol inhibits acetylcholine uptake in presynaptic vesicles and reduce its release. The present study was performed in order to test the effects of this drug in a cholinergic related function as rapid eye movement (REM) sleep. Wistar male rats were implanted for sleep recordings. In addition, a stainless steel cannula was implanted into the left lateral ventricle for intracerebroventricular (ICV) injections. In experiment 1, a dose-response curve was performed. Saline or vesamicol (20, 40, 80 and 100 micrograms) were injected. Following the ICV injections, animals' sleep was recorded for 8 h. In experiment 2, after adaptation and baseline recordings, animals received 50 micrograms vesamicol ICV at 1000 hours. every 24 h for 2 consecutive days. After each injection an 8-h sleep recording session was performed. Two subsequent recovery recordings were allowed. Results obtained in experiment 1 showed a dose-response reduction of REM sleep with significant values at 80 micrograms and 100 micrograms of vesamicol. The main findings in experiment 2 were a reduction in REM sleep time and an increase in REM sleep latency. On the recovery days, a dramatic rebound of REM sleep was observed. Vesamicol behaved as an anticholinergic drug. It produced a reduction in REM sleep time and a rebound of this sleep stage after its withdrawal.
authors.affiliation: Departamento de Fisiologia, Facultad de Medicina, Universidad Nacional Autonoma de Mexico, Mexico.
authors.forename: R J
authors.initials: RJ
authors.lastname: Salin-Pascual
authors.forename: A
authors.initials: A
authors.lastname: Jimenez-Anguiano
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D004305:Dose-Response Relationship, Drug; D008297:Male; D009467:Neuromuscular Depolarizing Agents / Q000494:pharmacology*; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012890:Sleep / Q000187:drug effects*; D012895:Sleep, REM / Q000187:drug effects*
chemical_list: D009467:Neuromuscular Depolarizing Agents; D010880:Piperidines; C006189:vesamicol