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.

Cholinergic axons regulate type I acini in salivary glands of Ixodes ricinus and Ixodes scapularis ticks

“…Therefore, we designed an experiment to test whether disrupting synaptic ACh release and/or blocking postsynaptic mAChR in type I acini may affect water ingestion in severely dehydrated ticks. Although we observed substantial variation in the amount of ingested water between individual Ixodes females, significantly less volume was ingested by ticks treated with vesamicol, a drug inhibiting ACh uptake by synaptic vesicles and thus reducing its release into the synapse 74 . Interestingly, ticks treated with the mAChR-A antagonist, atropine, ingested approximately the same volume of water as control ticks.…”

Covert REM sleep effects on REM mentation: Further methodological considerations and supporting evidence

“…The new presynaptic anticholinergic agents have been shown to block REM : Salin-Pascual et al 1995. The new presynaptic anticholinergic agents have been shown to block REM : Salin-Pascual et al 1995.…”

Imaging in vivo acetylcholine release in the peripheral nervous system with a fluorescent nanosensor

“…As a second confirmation of the response to ACh, an anticholinergic drug, vesamicol, was introduced to temporarily block the release of ACh. Vesamicol inhibits ACh release by inhibiting ACh uptake into synaptic vesicles in presynaptic neurons (47). We incubated the nanosensor-stained SMG with vesamicol for 10 min and recorded the sensor's response with electrical stimulation at 3 V. We then washed away the vesamicol and stimulated the lingual nerve under the same stimulation conditions.…”