RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats.
RP 62203, a naphtosultam derivative, is an antagonist at the 5-hydroxytryptamine2 (HT2) receptor. The sleep pattern of rats treated orally with RP 62203 was studied at doses ranging from 0.5 to 4 mg/kg. Following RP 62203 administration, the duration of deep nonrapid eye movement (NREM) sleep was found to increase at the expense of wakefulness in a dose-dependent manner from 0.5 mg/kg. The 5-HT2 receptor agonist DOI and the 5-HT1a receptor agonist 8 OH-DPAT induced a dose-related increase in wakefulness; treatment with RP 62203 reversed the enhancement of wakefulness produced by DOI but not that produced by 8 OH-DPAT. These data provide further evidence for the involvement of 5-HT2 receptors in the regulation of NREM sleep in rats. RP 62203 could therefore be of clinical interest in the management of sleep disorders, particularly those developing within a psychiatric context.
Stutzmann
J M
JM
Electrophysiology Department, Rhone Poulenc Rorer, Centre de Recherche de Vitry-Alfortville, Vitry sur Seine, France.
Eon
B
B
Lucas
M
M
Blanchard
J C
JC
Laduron
P M
PM
D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000502:physiology; D003499:Cyclic S-Oxides / Q000494:pharmacology*; D004569:Electroencephalography / Q000187:drug effects; D005260:Female; D006801:Humans; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology*; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects*; D016713:Ritanserin / Q000494:pharmacology; D012890:Sleep / Q000502:physiology; D012894:Sleep Stages / Q000187:drug effects* / Q000502:physiology; D012895:Sleep, REM / Q000187:drug effects / Q000502:physiology; D014851:Wakefulness
D003499:Cyclic S-Oxides; D009281:Naphthalenes; D011985:Receptors, Serotonin; D016713:Ritanserin; C070475:fananserin