WS0701: a novel sedative-hypnotic agent acting on the adenosine system.

摘要: To characterize the sedative and hypnotic profile of novel adenosine derivative ((3S,4R,5R)-3,4-dihydroxy-5-(6-((4-hydroxy-3-methoxybenzyl)amino)-9H-purin-9-yl)tetrahydrofuran-2-yl) methyl diaconate (WS0701), we performed a variety behavioural tests investigated influence WS0701 on various sleep stages. In mice, significantly increased number entries time spent in open arms elevated plus maze test, indicating an anxiolytic effect. decreased locomotor activity counts head dips hole-board test enhanced sodium pentobarbital-induced hypnosis. However, did not induce loss righting reflex or amnesic effects models. rats, exerted effect markedly prolonged non-rapid-eye-movement sleep, especially slow-wave but reduced rapid-eye-movement (REMS). Pretreatment with selective A2a receptor antagonist SCH58261 attenuated WS0701. protect mice against picrotoxin-induced seizures, inhibited deaminase levels frontal cortex hypothalamus mice. conclusion, shows anxiolytic, as well stage alterative effects, which may be related to system.