Selective blockade of different brain stem muscarinic receptor subtypes: effects on the sleep-wake cycle

Age-Related Effects of Scopolamine on REM Sleep Regulation in Normal Control Subjects Relationship to Sleep Abnormalities in Depression

“…While acute administration of muscarinic agonists can shorten REM latency, increase REM activity and REM density, and reduce slow-wave sleep (Berkowitz et al 1990;Riemann and Berger 1989;Riemann et al 1988;Sitaram and Gillin 1980;Sitaram et al 1977Sitaram et al , 1978, acute administration of muscarinic cholinergic antagonists generally produce the opposite effects (Gillin et al 1991b;Hohagen et al 1994;Poland et al 1989Poland et al , 1997Sagalés et al 1969;Salin-Pascual et al 1993;Sitaram et al 1978). Based upon the pharmacologic profile of the compounds used to manipulate sleep, it appears that both M1 and M2 muscarinic receptor subtypes are involved in the regulation of REM sleep and its various elements Imeri et al 1994;Velazquez-Moctezuma et al 1989, 1991Zoltoski et al 1993). The results from this study should be considered as preliminary findings due the modest sample sizes of the two groups.…”

Antidepressant and Antipsychotic Drugs

“…[20] Some of the arousal effects of acetylcholine appear to be mediated via muscarinic cholinergic receptors which are blocked by any antidepressant and antipsychotic medications, resulting in a decrease in arousal and promotion of sleep. [21]…”

Sleep, activity, temperature and arousal responses of mice deficient for muscarinic receptor M2 or M4

“…Muscarinic receptors have a well documented role in mediating the vigilance-related effects of acetylcholine (Baghdoyan and Lydic 1999;Brischoux et al 2008;Imeri et al 1994;Jones 2004). Two muscarinic receptors, types 2 and 4 (M2R and M4R) are both G-protein-coupled and differ from each other in their tissue distribution and their physiologic effects (Wess 2004).…”

“…Thus, cholinergic interactions between these structures link the regulation of arousal, the sleep/wake cycle, and sensorimotor gating as reflected in acoustic startle and prepulse inhibition (PPI) of acoustic startle. M2R has a well documented role in mediating the vigilance-related effects of acetylcholine in all of these regions (Baghdoyan and Lydic 1999;Coleman et al 2004;Imeri et al 1994). In addition, cholinergic influences may vary with regard to circadian and homeostatic components of sleep regulation (Schwartz and Roth 2008;Sinton and McCarley 2004).…”